Mirdametinib | PD0325901 | MEK Inhibitor | AmBeed-信号通路专用抑制剂

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Mirdametinib 99%+

货号：A370482 同义名： PD0325901;PD325901

PD0325901 is selective and non ATP-competitive MEK inhibitor with IC50 of 0.33 nM.

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type	HazMat fee for 500 gram (Estimated)
Excepted Quantity	USD 0.00
Limited Quantity	USD 15-60
Inaccessible (Haz class 6.1), Domestic	USD 80+
Inaccessible (Haz class 6.1), International	USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic	USD 100+
Accessible (Haz class 3, 4, 5 or 8), International	USD 200+

Mirdametinib 化学结构
CAS号：391210-10-9

Mirdametinib 3D分子结构
CAS号：391210-10-9

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Mirdametinib 纯度/质量文件产品仅供科研

货号：A370482 标准纯度： 99%+ 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024, 67(17): 14974-14985. Ambeed. [ A288696 ]; • JMC, 2024, 67(17): 15061-15079. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 更多 >

MEK 亚型比较

产品名称	MEK ↓ ↑	MEK1 ↓ ↑	MEK1/2 ↓ ↑	MEK2 ↓ ↑	MEK5 ↓ ↑	其他靶点	纯度
Honokiol	✔						98%
Mirdametinib	++++ MEK, IC50: 0.33 nM						99%+
Binimetinib	+++ MEK, IC50: 12 nM						99%+
BI-847325		++ MEK1, IC50: 25 nM		+++ MEK2, IC50: 4 nM			99%+
U0126-EtOH		+ MEK1, IC50: 0.07 μM		++ MEK2, IC50: 0.06 μM			98%
GDC-0623		++++ MEK1, IC50: 0.13 nM					99%+
TAK-733		++++ MEK1, IC50: 3.2 nM					99%+
Trametinib		++++ MEK1, IC50: 0.92 nM		++++ MEK2, IC50: 1.8 nM			99%+
Selumetinib		+++ MEK1, IC50: 14 nM MEK1, Kd: 99 nM		+ MEK2, Kd: 530 nM			99%+
CI-1040		++ MEK1, IC50: 17 nM		++ MEK2, IC50: 17 nM			99%+
Myricetin		✔					98%
Refametinib		++ MEK1, IC50: 19 nM		++ MEK2, IC50: 47 nM			99%+
Cobimetinib		+++ MEK1, IC50: 4.2 nM					99%+
PD98059		+ MEK1, IC50: 2 μM					99%+
SL327		+ MEK1, IC50: 0.18 μM		+ MEK2, IC50: 0.22 μM		AP-1	98+%
PD318088			✔				98%
AZD8330			+++ MEK1/2, IC50: 7 nM				99%+
Pimasertib							98%
(E/Z)-BIX02189					++++ MEK5, IC50: 1.5 nM		99%+
(E/Z)-BIX02188					+++ MEK5, IC50: 4.3 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Mirdametinib 生物活性

靶点	MEK MEK, IC50:0.33 nM
描述	MEKs, which are members of the MAPKK family, can activate both ERK1 and ERK2 by catalyzing the phosphorylation on T202/Y204. Also MEK itself can be phosphorylated and activated through Ras when the upstream signaling is activated by extracellular stimuli, including growth factors, hormones etc.. PD0325901 is a MEK1/2 with IC50 value of 0.33nM^[1]. PD0325901 showed more potency to cell lines harboring BRAF-mutation , including SKMEL28, SKMEL3, SKMEL19, SKMEL1, MALME3M, Colo205 and DU4475, with IC50 values below 10nM, compared with RAS/BRAF-WT cells with IC50>100nM. Meanwhile, dose-dependent decreased p-ERK and Cyclin D1 by PD0325901 can also be observed in these BRAF-mutant cells at concentration>10nM. These suggested that the BRAF mutation may confer the preferential sensitivity of cell lines to MEK inhibition by PD0325901. Consistent with the cellular studies, oral administration with PD0325901 suppressed the tumor growth in mice xenograft SKMEL28 harboring BRAF-V600E mutation at both dose of 5mg/kg and 25mg/kg, accompanied with decrease of p-ERK, Cyclin D1, RB and increased p27. In contrast, treatment with PD0325901 suppressed tumor growth in SKMEL31 (RAS/RAF-WT) xenografts only at high dose (25mg/kg) or even showed no effect in BT-474 (RAS/RAF-WT) xenografts at both dose, regardless the decreased p-ERK by PD0325901^[2]. Also it is found that PD0325901 can enhance generation of iPSCs^[3].
作用机制	PD0325901 is a derivative of CI-1040, which is a non-competitive inhibitor of MEK1/2.^[2]

Mirdametinib 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
human A101D cell		Growth inhibition assay		Inhibition of human A101D cell growth in a cell viability assay, IC50=11.45 nM.	SANGER
human A375 cell		Growth inhibition assay		Inhibition of human A375 cell growth in a cell viability assay, IC50=2.69 nM.	SANGER
human A375 cells		Proliferation assay	72 h	Antiproliferative activity against human A375 cells expressing BRAF V600E mutant after 72 hrs by Cell titer-glo assay, IC50=13 nM.	23474388
human A549 cell		Growth inhibition assay		Inhibition of human A549 cell growth in a cell viability assay, IC50=7.89 nM.	SANGER

Mirdametinib 动物研究

Dose

Pig: 0.79 mg/kg^[4] (p.o.)
Mice: 0.5 mg/kg, 1 mg/kg^[5] (i.p.), 1.5 mg/kg - 10 mg/kg^[6] (p.o.), 25 mg/kg^[7] (p.o.)
Rat: 10 mg/kg - 100 mg/kg^[8] (i.v., p.o.)

Administration

p.o., i.p., i.v.

Pharmacokinetics

Animal	Rats^[8]
Dose	30 mg/kg (i.v. or p.o.)
Administration	i.v. p.o.
C_max	129 µg/ml (i.v.) 16.9 µg/ml (p.o.)
T_max	1 h (p.o.)
AUC_0→24h	148 µg·h/ml (i.v..) 82.7 µg·h/ml (p.o.)

Mirdametinib 临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03170206	Lung Cancer	Phase 1 Phase 2	Recruiting	March 31, 2024	United States, Massachusetts ... 展开 >> Dana Farber Cancer Institute Recruiting Boston, Massachusetts, United States, 02215 Contact: Geoffrey Shapiro, MD, PhD 617-632-4942 Principal Investigator: Geoffrey Shapiro, MD Massachusetts General Hospital Not yet recruiting Boston, Massachusetts, United States, 02215 Contact: Rebecca Heist, MD 617-726-1838 Principal Investigator: Rebecca Heist, MD 收起 <<
NCT02510001	Solid Tumor C... 展开 >>olorectal Cancer 收起 <<	Phase 1	Active, not recruiting	September 2019	United Kingdom ... 展开 >> Oxford University Hospital NHS Trust Oxford, United Kingdom, OX3 7LE 收起 <<
NCT01347866	-		Terminated(Refer to Detailed D... 展开 >>escription for documentaion of Termination Statement.) 收起 <<	-	-

Mirdametinib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.07mL

0.41mL

0.21mL

10.37mL

2.07mL

1.04mL

20.74mL

4.15mL

2.07mL

Mirdametinib 技术信息

CAS号	391210-10-9
分子式	C₁₆H₁₄F₃IN₂O₄
分子量	482.193

别名	PD0325901;PD325901
运输	蓝冰

存储条件

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 55 mg/mL(114.06 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

5%DMSO+40%PEG300+5%Tween80+50%water 5 mg/mL

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摩尔计算器

计算溶液所需的质量，体积或浓度。 Ambeed 摩尔浓度计算器基于以下方程式：

浓度 (mol/L) × 体积 (L) × 分子量 (g/mol)=质量 (g)

浓度

体积

分子量

质量

*在制备母液时，请始终参考产品标签或 MSDS / COA（在产品页面可下载）上所显示的对应批次产品的分子量。

靶点

靶点	数值

MEK	MEK, IC50:0.33 nM

总药量计算器

动物实验：给药剂量 mg/kg 动物体重 g 动物数量只每天给药次给药天

需要的总药量： mg

工作液计算器

动物实验：给药剂量 mg/kg 动物体重 g 给药体积 μL

您需要配制的工作液浓度为：mg/mL

细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源

human A101D cell		Growth inhibition assay		Inhibition of human A101D cell growth in a cell viability assay, IC50=11.45 nM.	SANGER
human A375 cell		Growth inhibition assay		Inhibition of human A375 cell growth in a cell viability assay, IC50=2.69 nM.	SANGER
human A375 cells		Proliferation assay	72 h	Antiproliferative activity against human A375 cells expressing BRAF V600E mutant after 72 hrs by Cell titer-glo assay, IC50=13 nM.	23474388
human A549 cell		Growth inhibition assay		Inhibition of human A549 cell growth in a cell viability assay, IC50=7.89 nM.	SANGER
human ABC-1 cell		Growth inhibition assay		Inhibition of human ABC-1 cell growth in a cell viability assay, IC50=123.02 nM.	SANGER
human ACN cell		Growth inhibition assay		Inhibition of human ACN cell growth in a cell viability assay, IC50=15.76 nM.	SANGER
human AGS cell		Growth inhibition assay		Inhibition of human AGS cell growth in a cell viability assay, IC50=20.41 nM.	SANGER
human AsPC-1 cell		Growth inhibition assay		Inhibition of human AsPC-1 cell growth in a cell viability assay, IC50=45.28 nM.	SANGER
human BB30-HNC cell		Growth inhibition assay		Inhibition of human BB30-HNC cell growth in a cell viability assay, IC50=85.51 nM.	SANGER
human BHT-101 cell		Growth inhibition assay		Inhibition of human BHT-101 cell growth in a cell viability assay, IC50=6.7 nM.	SANGER
human BPH-1 cell		Growth inhibition assay		Inhibition of human BPH-1 cell growth in a cell viability assay, IC50=3.95 nM.	SANGER
human C2BBe1 cell		Growth inhibition assay		Inhibition of human C2BBe1 cell growth in a cell viability assay, IC50=28.54 nM.	SANGER
human C32 cell		Growth inhibition assay		Inhibition of human C32 cell growth in a cell viability assay, IC50=3.67 nM.	SANGER
human CAL-27 cell		Growth inhibition assay		Inhibition of human CAL-27 cell growth in a cell viability assay, IC50=44.91 nM	SANGER
human CAL-39 cell		Growth inhibition assay		Inhibition of human CAL-39 cell growth in a cell viability assay, IC50=39.04 nM.	SANGER
human CAL-62 cell		Growth inhibition assay		Inhibition of human CAL-62 cell growth in a cell viability assay, IC50=100.78 nM.	SANGER
human CHP-212 cell		Growth inhibition assay		Inhibition of human CHP-212 cell growth in a cell viability assay, IC50=0.527 nM.	SANGER
human COLO-679 cell		Growth inhibition assay		Inhibition of human COLO-679 cell growth in a cell viability assay, IC50=10.01 nM	SANGER
human COLO-741 cell		Growth inhibition assay		Inhibition of human COLO-741 cell growth in a cell viability assay, IC50=7.1 nM.	SANGER
human COLO-792 cell		Growth inhibition assay		Inhibition of human COLO-792 cell growth in a cell viability assay, IC50=43.15 nM.	SANGER
human COR-L105 cell		Growth inhibition assay		Inhibition of human COR-L105 cell growth in a cell viability assay, IC50=71.71 nM.	SANGER
human CP50-MEL-B cell		Growth inhibition assay		Inhibition of human CP50-MEL-B cell growth in a cell viability assay, IC50=4.58 nM.	SANGER
human DOK cell		Growth inhibition assay		Inhibition of human DOK cell growth in a cell viability assay, IC50=13.4 nM.	SANGER
human DU-4475 cell		Growth inhibition assay		Inhibition of human DU-4475 cell growth in a cell viability assay, IC50=3.57 nM.	SANGER
human EGI-1 cell		Growth inhibition assay		Inhibition of human EGI-1 cell growth in a cell viability assay, IC50=95.81 nM.	SANGER
human EM-2 cell		Growth inhibition assay		Inhibition of human EM-2 cell growth in a cell viability assay, IC50=74.7 nM.	SANGER
human GAK cell		Growth inhibition assay		Inhibition of human GAK cell growth in a cell viability assay, IC50=66.87 nM.	SANGER
human H9 cell		Growth inhibition assay		Inhibition of human H9 cell growth in a cell viability assay, IC50=5.77 nM.	SANGER
human HCC1419 cell		Growth inhibition assay		Inhibition of human HCC1419 cell growth in a cell viability assay, IC50=91.38 nM.	SANGER
human HCC2998 cell		Growth inhibition assay		Inhibition of human HCC2998 cell growth in a cell viability assay, IC50=33.66 nM.	SANGER
human HCC70 cell		Growth inhibition assay		Inhibition of human HCC70 cell growth in a cell viability assay, IC50=63.01 nM.	SANGER
human HD-MY-Z cell		Growth inhibition assay		Inhibition of human HD-MY-Z cell growth in a cell viability assay, IC50=71.12 nM.	SANGER
human H-EMC-SS cell		Growth inhibition assay		Inhibition of human H-EMC-SS cell growth in a cell viability assay, IC50=11.02 nM.	SANGER
human HL-60 cell		Growth inhibition assay		Inhibition of human HL-60 cell growth in a cell viability assay, IC50=11.15 nM.	SANGER
human HN cell growth		Growth inhibition assay		Inhibition of human HN cell growth in a cell viability assay, IC50=122.59 nM.	SANGER
human HO-1-N-1 cell		Growth inhibition assay		Inhibition of human HO-1-N-1 cell growth in a cell viability assay, IC50=34.43 nM.	SANGER
human Hs-578-T cell		Growth inhibition assay		Inhibition of human Hs-578-T cell growth in a cell viability assay, IC50=12.79 nM.	SANGER
human HT-1080 cell		Growth inhibition assay		Inhibition of human HT-1080 cell growth in a cell viability assay, IC50=85.88 nM.	SANGER
human HT-144 cell		Growth inhibition assay		Inhibition of human HT-144 cell growth in a cell viability assay, IC50=8.97 nM.	SANGER
human HT-29 cell		Growth inhibition assay		Inhibition of human HT-29 cell growth in a cell viability assay, IC50=50.49 nM.	SANGER
human HTC-C3 cell		Growth inhibition assay		Inhibition of human HTC-C3 cell growth in a cell viability assay, IC50=5.89 nM.	SANGER
human HuP-T3 cell		Growth inhibition assay		Inhibition of human HuP-T3 cell growth in a cell viability assay, IC50=83.93 nM.	SANGER
human HuP-T4 cell		Growth inhibition assay		Inhibition of human HuP-T4 cell growth in a cell viability assay, IC50=10.98 nM.	SANGER
human IA-LM cell		Growth inhibition assay		Inhibition of human IA-LM cell growth in a cell viability assay, IC50=73.28 nM.	SANGER
human KNS-62 cell		Growth inhibition assay		Inhibition of human KNS-62 cell growth in a cell viability assay, IC50=69.99 nM.	SANGER
human KY821 cell		Growth inhibition assay		Inhibition of human KY821 cell growth in a cell viability assay, IC50=53.3 nM.	SANGER
human LAMA-84 cell		Growth inhibition assay		Inhibition of human LAMA-84 cell growth in a cell viability assay, IC50=94.68 nM.	SANGER
human LB1047-RCC cell		Growth inhibition assay		Inhibition of human LB1047-RCC cell growth in a cell viability assay, IC50=59.65 nM.	SANGER
human LB2241-RCC cell		Growth inhibition assay		Inhibition of human LB2241-RCC cell growth in a cell viability assay, IC50=65.52 nM.	SANGER
human LB2518-MEL cell		Growth inhibition assay		Inhibition of human LB2518-MEL cell growth in a cell viability assay, IC50=11.13 nM.	SANGER
human LoVo cell		Growth inhibition assay		Inhibition of human LoVo cell growth in a cell viability assay, IC50=65.29 nM.	SANGER
human LOXIMVI cell		Growth inhibition assay		Inhibition of human LOXIMVI cell growth in a cell viability assay, IC50=39.39 nM.	SANGER
human LS-513 cell		Growth inhibition assay		Inhibition of human LS-513 cell growth in a cell viability assay, IC50=114.83 nM.	SANGER
human M14 cell		Growth inhibition assay		Inhibition of human M14 cell growth in a cell viability assay, IC50=1.45 nM.	SANGER
human MCF7 cells		Function assay	75 mins	Inhibition of MEk1/2 in human MCF7 cells assessed as decrease in ERK phosphorylation after 75 mins by Western blotting analysis	23398453
human MDA-MB-175-VII cell		Growth inhibition assay		Inhibition of human MDA-MB-175-VII cell growth in a cell viability assay	SANGER
human MEG-01 cell		Growth inhibition assay		Inhibition of human MEG-01 cell growth in a cell viability assay, IC50=97.77 nM.	SANGER
human MEL-HO cell		Growth inhibition assay		Inhibition of human MEL-HO cell growth in a cell viability assay, IC50=9.49 nM.	SANGER
human Mewo cell		Growth inhibition assay		Inhibition of human Mewo cell growth in a cell viability assay, IC50=14.45 nM.	SANGER
human MIA-PaCa-2 cell		Growth inhibition assay		Inhibition of human MIA-PaCa-2 cell growth in a cell viability assay, IC50=63.53 nM.	SANGER
human MIAPaCa2 cells		Proliferation assay		Antiproliferative activity against human MIAPaCa2 cells, IC50=17 nM.	23474388
human MV-4-11 cell		Growth inhibition assay		Inhibition of human MV-4-11 cell growth in a cell viability assay, IC50=94.73 nM.	SANGER
human MZ2-MEL cell		Growth inhibition assay		Inhibition of human MZ2-MEL cell growth in a cell viability assay, IC50=35.65 nM.	SANGER
human MZ7-mel cell		Growth inhibition assay		Inhibition of human MZ7-mel cell growth in a cell viability assay, IC50=29.43 nM.	SANGER
human NB10 cell		Growth inhibition assay		Inhibition of human NB10 cell growth in a cell viability assay, IC50=100.42 nM.	SANGER
human NB69 cell		Growth inhibition assay		Inhibition of human NB69 cell growth in a cell viability assay	SANGER
human NCI-H1437 cell		Growth inhibition assay		Inhibition of human NCI-H1437 cell growth in a cell viability assay, IC50=34.49 nM.	SANGER
human NCI-H1666 cell		Growth inhibition assay		Inhibition of human NCI-H1666 cell growth in a cell viability assay, IC50=11.17 nM.	SANGER
human NCI-H2087 cell		Growth inhibition assay		Inhibition of human NCI-H2087 cell growth in a cell viability assay, IC50=101.14 nM.	SANGER
human NCI-H2291 cell		Growth inhibition assay		Inhibition of human NCI-H2291 cell growth in a cell viability assay, IC50=46.46 nM.	SANGER
human NCI-H292 cell		Growth inhibition assay		Inhibition of human NCI-H292 cell growth in a cell viability assay, IC50=47.39 nM.	SANGER
human NCI-H747 cell		Growth inhibition assay		Inhibition of human NCI-H747 cell growth in a cell viability assay, IC50=34.98 nM.	SANGER
human NCI-SNU-1 cell		Growth inhibition assay		Inhibition of human NCI-SNU-1 cell growth in a cell viability assay, IC50=96.73 nM.	SANGER
human NOMO-1 cell		Growth inhibition assay		Inhibition of human NOMO-1 cell growth in a cell viability assay, IC50=2.07 nM.	SANGER
human OMC-1 cell		Growth inhibition assay		Inhibition of human OMC-1 cell growth in a cell viability assay, IC50=100.23 nM.	SANGER
human ONS-76 cell		Growth inhibition assay		Inhibition of human ONS-76 cell growth in a cell viability assay, IC50=14.51 nM.	SANGER
human OVCAR-5 cell		Growth inhibition assay		Inhibition of human OVCAR-5 cell growth in a cell viability assay, IC50=7.82 nM.	SANGER
human P12-ICHIKAWA cell		Growth inhibition assay		Inhibition of human P12-ICHIKAWA cell growth in a cell viability assay, IC50=62.27 nM.	SANGER
human PANC1 cells	10 μM	Function assay	1 h	Inhibition of MEK1 in human PANC1 cells assessed as reduction in pErk1/2 level at 10 uM after 1 hr by Western blotting analysis	25766633
human PSN1 cell		Growth inhibition assay		Inhibition of human PSN1 cell growth in a cell viability assay, IC50=38.45 nM	SANGER
human RCM-1 cell		Growth inhibition assay		Inhibition of human RCM-1 cell growth in a cell viability assay, IC50=46.85 nM.	SANGER
human RD cell		Growth inhibition assay		Inhibition of human RD cell growth in a cell viability assay, IC50=67.1 nM.	SANGER
human RKO cell growth		Growth inhibition assay		Inhibition of human RKO cell growth in a cell viability assay, IC50=52.02 nM.	SANGER
human RMG-I cell		Growth inhibition assay		Inhibition of human RMG-I cell growth in a cell viability assay, IC50=87.34 nM.	SANGER
human RT-112 cell		Growth inhibition assay		Inhibition of human RT-112 cell growth in a cell viability assay, IC50=48.84 nM.	SANGER
human RVH-421 cell		Growth inhibition assay		Inhibition of human RVH-421 cell growth in a cell viability assay, IC50=12.64 nM.	SANGER
human SH-4 cell growth		Growth inhibition assay		Inhibition of human SH-4 cell growth in a cell viability assay, IC50=8.26 nM.	SANGER
human SJSA-1 cell		Growth inhibition assay		Inhibition of human SJSA-1 cell growth in a cell viability assay, IC50=123.19 nM.	SANGER
human SK-MEL-2 cell		Growth inhibition assay		Inhibition of human SK-MEL-2 cell growth in a cell viability assay, IC50=35.2 nM.	SANGER
human SK-MEL-28 cell		Growth inhibition assay		Inhibition of human SK-MEL-28 cell growth in a cell viability assay, IC50=1.52 nM.	SANGER
human SK-N-AS cell		Growth inhibition assay		Inhibition of human SK-N-AS cell growth in a cell viability assay, IC50=8.44 nM.	SANGER
human SNU-387 cell		Growth inhibition assay		Inhibition of human SNU-387 cell growth in a cell viability assay, IC50=93.36 nM	SANGER
human SW1116 cell		Growth inhibition assay		Inhibition of human SW1116 cell growth in a cell viability assay, IC50=60.49 nM.	SANGER
human SW620 cell		Growth inhibition assay		Inhibition of human SW620 cell growth in a cell viability assay, IC50=14.95 nM.	SANGER
human SW626 cell		Growth inhibition assay		Inhibition of human SW626 cell growth in a cell viability assay, IC50=14.91 nM.	SANGER
human SW756 cell		Growth inhibition assay		Inhibition of human SW756 cell growth in a cell viability assay, IC50=34.45 nM.	SANGER
human SW780 cell		Growth inhibition assay		Inhibition of human SW780 cell growth in a cell viability assay, IC50=92.32 nM.	SANGER
human SW872 cell		Growth inhibition assay		Inhibition of human SW872 cell growth in a cell viability assay, IC50=27.99 nM.	SANGER
human T-24 cell		Growth inhibition assay		Inhibition of human T-24 cell growth in a cell viability assay, IC50=19.71 nM.	SANGER
human TYK-nu cell		Growth inhibition assay		Inhibition of human TYK-nu cell growth in a cell viability assay, IC50=15.13 nM.	SANGER
human UACC-257 cell		Growth inhibition assay		Inhibition of human UACC-257 cell growth in a cell viability assay, IC50=14.62 nM.	SANGER
human WM-115 cell		Growth inhibition assay		Inhibition of human WM-115 cell growth in a cell viability assay, IC50=48.5 nM.	SANGER

临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT03170206	Lung Cancer	Phase 1 Phase 2	Recruiting	March 31, 2024	United States, Massachusetts ... 展开 >> Dana Farber Cancer Institute Recruiting Boston, Massachusetts, United States, 02215 Contact: Geoffrey Shapiro, MD, PhD 617-632-4942 Principal Investigator: Geoffrey Shapiro, MD Massachusetts General Hospital Not yet recruiting Boston, Massachusetts, United States, 02215 Contact: Rebecca Heist, MD 617-726-1838 Principal Investigator: Rebecca Heist, MD 收起 <<
NCT02510001	Solid Tumor C... 展开 >>olorectal Cancer 收起 <<	Phase 1	Active, not recruiting	September 2019	United Kingdom ... 展开 >> Oxford University Hospital NHS Trust Oxford, United Kingdom, OX3 7LE 收起 <<
NCT01347866	-		Terminated(Refer to Detailed D... 展开 >>escription for documentaion of Termination Statement.) 收起 <<	-	-
NCT01347866	Advanced Cancer	Phase 1	Terminated(Refer to Detailed D... 展开 >>escription for documentaion of Termination Statement.) 收起 <<	-	United States, California ... 展开 >> Ronald Reagan UCLA Medical Center Los Angeles, California, United States, 90095-6984 Ronald Reagan UCLA Medical Center Los Angeles, California, United States, 90095 UCLA Medical Center Los Angeles, California, United States, 90095 UCLA Oncology Center Los Angeles, California, United States, 90095 Santa Monica - UCLA Medical Center and Orthopaedic Hospital Santa Monica, California, United States, 90404 UCLA Santa Monica Hematology Oncology Santa Monica, California, United States, 90404 United States, Colorado Anschutz Cancer Pavilion Aurora, Colorado, United States, 80045 University of Colorado Denver (CTRC) Aurora, Colorado, United States, 80045 University of Colorado Hospital Anschutz Inpatient Pavilion Aurora, Colorado, United States, 80045 University of Colorado Hospital Aurora, Colorado, United States, 80045 United States, South Carolina Medical University of South Carolina, Hollings Cancer Center Charleston, South Carolina, United States, 29425 Medical University of South Carolina Charleston, South Carolina, United States, 29425 MUSC, Investigational Drug Services Charleston, South Carolina, United States, 29425 MUSC Health East Cooper Mount Pleasant, South Carolina, United States, 29464 MUSC Specialty Care-North North Charleston, South Carolina, United States, 29406 Canada, Ontario Princess Margaret Hospital Toronto, Ontario, Canada, M5G 2M9 Italy Ospedale San Raffaele Milano, Italy, 20132 Spain Hospital General Vall d'Hebron Barcelona, Spain, 08035 收起 <<
NCT00147550	Melanoma Colo... 展开 >>nic Neoplasms Breast Neoplasms 收起 <<	Phase 1 Phase 2	Terminated(See termination rea... 展开 >>son in detailed description.) 收起 <<	-	United States, Alabama ... 展开 >> Pfizer Investigational Site Birmingham, Alabama, United States, 35233-2115 Pfizer Investigational Site Birmingham, Alabama, United States, 35233 Pfizer Investigational Site Birmingham, Alabama, United States, 35294 United States, California Pfizer Investigational Site La Jolla, California, United States, 92037 Pfizer Investigational Site La Jolla, California, United States, 92093 Pfizer Investigational Site La Mesa, California, United States, 91942 Pfizer Investigational Site Los Angeles, California, United States, 90025 Pfizer Investigational Site San Diego, California, United States, 92103 Pfizer Investigational Site San Diego, California, United States, 92123 Pfizer Investigational Site Santa Monica, California, United States, 90404 United States, Florida Pfizer Investigational Site Tampa, Florida, United States, 33612 United States, Michigan Pfizer Investigational Site Detroit, Michigan, United States, 48201 Pfizer Investigational Site Detroit, Michigan, United States, 48202 United States, Minnesota Pfizer Investigational Site Rochester, Minnesota, United States, 55905 United States, New York Pfizer Investigational Site New York, New York, United States, 10021 Pfizer Investigational Site New York, New York, United States, 10022 United States, Ohio Pfizer Investigational Site Cleveland, Ohio, United States, 44106 收起 <<
NCT00174369	Carcinoma, Non-Small-Cell Lung	Phase 2	Terminated(Terminated [See Det... 展开 >>ailed Description for Termination Reason.]) 收起 <<	-	United States, California ... 展开 >> Pfizer Investigational Site Greenbrae, California, United States, 94904 Pfizer Investigational Site La Jolla, California, United States, 92093 Pfizer Investigational Site LaJolla, California, United States, 92037 Pfizer Investigational Site San Diego, California, United States, 92103 Pfizer Investigational Site San Mateo, California, United States, 94402 United States, Florida Pfizer Investigational Site Tampa, Florida, United States, 33612 United States, Michigan Pfizer Investigational Site Ann Arbor, Michigan, United States, 48106-0995 Pfizer Investigational Site Detroit, Michigan, United States, 48201 Pfizer Investigational Site Farmington Hills, Michigan, United States, 48334 United States, Minnesota Pfizer Investigational Site Coon Rapids, Minnesota, United States, 55433 Pfizer Investigational Site Fridley, Minnesota, United States, 55432 Pfizer Investigational Site Robbinsdale, Minnesota, United States, 55422 United States, New York Pfizer Investigational Site New York, New York, United States, 11725 United States, Pennsylvania Pfizer Investigational Site Philadelphia, Pennsylvania, United States, 19111 收起 <<
NCT02297802	-		-	-	United States, California ... 展开 >> Sharp Healthcare San Diego, California, United States, 92123 收起 <<
NCT02039336	Colorectal Cancer	Phase 1 Phase 2	Recruiting	December 2019	Netherlands ... 展开 >> The Netherlands Cancer Institute Recruiting Amsterdam, Netherlands, 1066CX Contact: F opdam, MD, PhD +31 20 512 2446 f.opdam@nki.nl Erasmus Medical Center Cancer Institute Recruiting Rotterdam, Netherlands, 3015CE University Medical Center Utrecht Recruiting Utrecht, Netherlands, 3584CX 收起 <<
NCT02096471	Neurofibromatosis Type 1 and G... 展开 >>rowing or Symptomatic, Inoperable PN 收起 <<	Phase 2	Active, not recruiting	December 2018	United States, California ... 展开 >> Children's Hospital Los Angeles Los Angeles, California, United States, 90027 United States, District of Columbia Children's National Medical Center Washington, District of Columbia, United States, 20010 United States, Illinois University of Chicago Chicago, Illinois, United States, 60637 United States, Indiana Indiana Unversity Indianapolis, Indiana, United States, 46202 United States, Maryland National Cancer Institute (NCI) Bethesda, Maryland, United States, 20892 United States, Massachusetts Children's Hospital Boston Boston, Massachusetts, United States, 02115 United States, Missouri Washington University - St. Louis Saint Louis, Missouri, United States, 63110 United States, New York New York University Medical Center New York, New York, United States, 10016 United States, Ohio Cincinnati Children's Hospital Medical Center Cincinnati, Ohio, United States, 45229 United States, Pennsylvania Children's Hospital of Philadelphia Philadelphia, Pennsylvania, United States, 19096 United States, Utah University of Utah Salt Lake City, Utah, United States, 84132 收起 <<
NCT02022982	KRAS Mutant Non-Small Cell Lun... 展开 >>g Cancer Solid Tumors 收起 <<	Phase 1 Phase 2	Active, not recruiting	December 2020	United States, Massachusetts ... 展开 >> Dana Farber Cancer Institute Boston, Massachusetts, United States, 02115 收起 <<

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