Milciclib | CDK/TRK Inhibitor | AmBeed-信号通路专用抑制剂

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Milciclib {[allProObj[0].p_purity_real_show]}

货号：A127625 同义名： PHA-848125

Milciclib是一种强效的 ATP 竞争性 CDK 抑制剂，IC50 对 CDK2 为 45 nM，对 TRKA 为 53 nM，并能通过自噬诱导细胞死亡。

Milciclib 化学结构
CAS号：802539-81-7

Milciclib 3D分子结构
CAS号：802539-81-7

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Milciclib 纯度/质量文件产品仅供科研

货号：A127625 标准纯度： {[allProObj[0].p_purity_real_show]} 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: • JMC, 2024. Ambeed. [ A919389 , A918471 , A995972 ]; • Anal. Chem., 2024, 96(50): 19947-19954. Ambeed. [ A261947 , A1165388 ]; • ACS Biomater. Sci. Eng., 2024. Ambeed. [ A220462 ]; • ACS Biomater. Sci. Eng., 2024. Ambeed. [ A165235 , A110205 ]; • Pharmaceutics, 2024, 16(12): 1546. Ambeed. [ A272538 , A187261 , A691302 , A506702 ]; 更多 >

CDK 亚型比较

产品名称	Cdc ↓ ↑	CDK1 ↓ ↑	CDK19 ↓ ↑	CDK2 ↓ ↑	CDK3 ↓ ↑	CDK4 ↓ ↑	CDK5 ↓ ↑	CDK6 ↓ ↑	CDK7 ↓ ↑	CDK8 ↓ ↑	CDK9 ↓ ↑	CLK ↓ ↑	其他靶点	纯度
XL413 hydrochloride	++++ Cdc7, IC50: 3.4 nM													99%+
SU9516		+++ CDK1, IC50: 40 nM		+++ CDK2, IC50: 22 nM		++ CDK4, IC50: 200 nM								99%+
RO-3306		+++ CDK1, Ki: 20 nM											ERK,SGK	98%
R547		++++ CDK1/CyclinB, Ki: 2 nM		++++ CDK2/CyclinE, Ki: 3 nM		++++ CDK4/CyclinD1, Ki: 1 nM								99%+
BMS-265246		++++ CDK1/CyclinB, IC50: 6 nM		++++ CDK2/CyclinE, IC50: 9 nM		+ CDK4/CyclinD, IC50: 230 nM								99%+
NU6027		+ CDK1, Ki: 2.5 μM		+ CDK2, Ki: 1.3 μM									DNA-PK	98%
Purvalanol A	++++ Cdc2/CyclinB, IC50: 4 nM			+++ CDK2/CyclinE, IC50: 35 nM CDK2/CyclinA, IC50: 70 nM		+ CDK4/CyclinD1, IC50: 850 nM								99%+
SCH900776				++ CDK2, IC50: 0.16 μM										99%+
AUZ 454				++++ CDK2(C118L), Kd: 18.6 nM CDK2(A144C), Kd: 9.7 nM										99%+
A-674563 HCl				++ CDK2, Ki: 46 nM									PKA	99%
JNJ-7706621		++++ CDK1/CyclinB, IC50: 9 nM		++++ CDK2/CyclinE, IC50: 3 nM CDK2/CyclinA, IC50: 4 nM	++ CDK3/CyclinE, IC50: 58 nM	+ CDK4/CyclinD1, IC50: 253 nM		++ CDK6/CyclinD1, IC50: 175 nM						99%+
AT7519		++ CDK1/CyclinB, IC50: 210 nM		++ CDK2/CyclinA, IC50: 47 nM	+ CDK3/CyclinE, IC50: 360 nM	++ CDK4/CyclinD1, IC50: 100 nM	+++ CDK5/p35, IC50: 13 nM	++ CDK6/CyclinD3, IC50: 170 nM			++++ CDK9/CyclinT, IC50: <10 nM			98+%
PHA-793887		++ CDK1/CyclinB, IC50: 60 nM		++++ CDK2/CyclinE, IC50: 8 nM CDK2/CyclinA, IC50: 8 nM		++ CDK4/CyclinD1, IC50: 62 nM	++++ CDK5/p25, IC50: 5 nM		++++ CDK7/CyclinH, IC50: 10 nM		++ CDK9/CyclinT1, IC50: 138 nM			99%+
Milciclib		+ CDK1/CyclinB, IC50: 398 nM		++ CDK2/CyclinE, IC50: 363 nM CDK2/CyclinA, IC50: 45 nM		++ CDK4/CyclinD1, IC50: 160 nM	+ CDK5/p35, IC50: 265 nM		++ CDK7/CyclinH, IC50: 150 nM					99%+
Kenpaullone		+ CDK1/CyclinB, IC50: 0.4μM		+ CDK2/CyclinE, IC50: 7.5μM CDK2/CyclinA, IC50: 0.68μM			+ CDK5/p35, IC50: 0.85μM							98%
SNS-032				+++ CDK2/CyclinE, IC50: 48 nM CDK2/CyclinA, IC50: 38 nM			+ CDK5/p35, IC50: 340 nM		++ CDK7/CyclinH, IC50: 62 nM		++++ CDK9/CyclinT, IC50: 4 nM			99%+
Dinaciclib		++++ CDK1, IC50: 3 nM		++++ CDK2, IC50: 1 nM			++++ CDK5, IC50: 1 nM				++++ CDK9, IC50: 4 nM			99%+
PHA-767491 hydrochloride	++++ Cdc7, IC50: 10 nM	+ CDK1, IC50: 250 nM		+ CDK2, IC50: 240 nM			+ CDK5, IC50: 460 nM				+++ CDK9, IC50: 34 nM		MK2	99%
(R)-Roscovitine	+ Cdc2/CyclinB, IC50: 0.65 μM			+ CDK2/CyclinE, IC50: 0.7 μM CDK2/CyclinA, IC50: 0.7 μM			++ CDK5/p35, IC50: 0.16 μM							99%+
Narazaciclib						++++ CDK4/CyclinD1, IC50: 3.87 nM		++++ CDK6/CyclinD1, IC50: 9.82 nM					RET	99%+
Palbociclib						++++ CDK4/CyclinD1, IC50: 11 nM CDK4/CyclinD3, IC50: 9 nM		+++ CDK6/CyclinD2, IC50: 15 nM						99%
Abemaciclib						++++ CDK4, IC50: 2 nM		++++ CDK6, IC50: 10 nM						99%
Ribociclib						++++ CDK4, IC50: 10 nM		+++ CDK6, IC50: 39 nM						98%
Palbociclib isethionate						++++ CDK4/CyclinD1, IC50: 11 nM CDK4/CyclinD3, IC50: 9 nM		+++ CDK6/CyclinD2, IC50: 15 nM						99%+
BS-181 HCl									+++ CDK7, IC50: 21 nM					99%+
(E/Z)-THZ1 dihydrochloride									++++ CDK7, IC50: 3.2 nM					99%+
LDC4297									++++ CDK7, IC50: 0.13 nM					99%+
Senexin A			+ CDK19, Kd: 0.31 μM							+ CDK8, Kd: 0.83 μM				99%
MSC2530818										++++ CDK8, IC50: 2.6 nM				99%+
Wogonin											✔			99%+
Riviciclib HCl		++ CDK1/CyclinB, IC50: 79 nM		+ CDK2/CyclinE, IC50: 2.54 μM CDK2/CyclinA, IC50: 224 nM		++ CDK4/CyclinD1, IC50: 63 nM		+ CDK6/CyclinD3, IC50: 396 nM	+ CDK7/CyclinH, IC50: 2.87 μM		+++ CDK9/CyclinT1, IC50: 20 nM			99+%
LDC000067				+ CDK2, IC50: 2.441 μM							++ CDK9, IC50: 44 nM			98%
Flavopiridol		+++ CDK1, IC50: 40 nM		+++ CDK2, IC50: 40 nM		+++ CDK4, IC50: 40 nM		+++ CDK6, IC50: 40 nM	+ CDK7, IC50: 300 nM		+++ CDK9, IC50: 20 nM			99%+
LY2857785									+ CDK7, IC50: 0.246 μM	+++ CDK8, IC50: 0.016 μM	+++ CDK9, IC50: 0.011 μM			99%+
AZD-5438		+++ CDK1, IC50: 16 nM		++++ CDK2, IC50: 6 nM							+++ CDK9, IC50: 20 nM			99%+
ML167												++ CLK4, IC50: 136 nM Dyrk1B , IC50: 1648 nM		99%+
(E/Z)-TG003												+++ mCLK1, IC50: 200 nM mCLK4, IC50: 15 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。

Milciclib 生物活性

靶点	CDK5 CDK5/p35, IC50:265 nM CDK4 CDK4/CyclinD1, IC50:160 nM CDK2 CDK2/CyclinE, IC50:363 nM CDK2/CyclinA, IC50:45 nM CDK7 CDK7/CyclinH, IC50:150 nM CDK1 CDK1/CyclinB, IC50:398 nM
描述	Cyclin-dependent kinases (CDKs) are a family of protein kinases which along with their regulatory subunit cyclins play a key role in the growth, development, proliferation and death of eukaryotic cells and are responsible for insuring integrity in the coordination of events through the cell cycle ^[3]. PHA-848125 is a potent, dual inhibitor of CDK and Tropomyosin receptor kinase (TRK), with IC50s of 45, 150, 160, 363, 398 nM and 53 nM for cyclin A/CDK2, cyclin H/CDK7, cyclin D1/CDK4, cyclin E/CDK2, cyclin B/CDK1 and TRKA, respectively ^[4]. PHA-848125 (0.156 or 0.625 μM) up-regulates the expression of PDCD4, DDIT4, SESN2/sestrin 2 and DEPDC6/DEPTOR in GL-Mel cells ^[4]. PHA-848125 induces a clear accumulation of cells in G1 phase and it strongly inhibits NGF (nerve growth factor)-induced phosphorylation of TRKA (tropomyosin receptor kinase) in a dose-dependent manner ^[5]. PHA-848125 has significant antitumor activity in various human xenografts and carcinogen-induced tumors as well as in disseminated primary leukemia models, with plasma concentrations in rodents in the same range as those found active in inhibiting cancer cell proliferation. PHA-848125 (5, 10, and 15 mg/kg, p.o.) inhibits the growth of tumor in 7, 12-dimethylbenz anthracene (DMBA)-induced rat mammary carcinoma model ^[5].
作用机制	PHA-848125 is a potent, ATP-competitive CDK inhibitor for CDK2 with IC50 of 45 nM, being > 3-fold selective for CDK2 than CDK1, 2, 4, 5, and 7.

Milciclib 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 A2780 cells		Proliferation assay	72 h	Antiproliferative activity against human A2780 cells after 72 hrs by cell Titer_Glo assay, IC50=0.2 μM	19603809
human A2780 cells		Function assay		Inhibition of CDK2 in human A2780 cells assessed as reduction of hyperphosphorylated form of retinoblastoma protein at 1 uM relative to control	19603809

Milciclib 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
NCT03109886	Hepatocellular Carcinoma	Phase 2	Active, not recruiting	August 2019	Greece ... 展开 >> Ippokrateio General Hospital of Athens Athens, Greece, 11527 Laiko General Hospital of Athens Athens, Greece, 11527 General University Hospital of Larissa Larissa, Greece, 41110 University General Hospital of Thessaloniki - AHEPA Thessaloniki, Greece, 54636 Israel Rambam Health Corporation Haifa, Israel, 31096 Rabin Medical Center - Beilinson Hospital Petah Tikva, Israel, 4941492 The Sheba Academic Medical Center Hospital - Tel Hashomer Ramat Gan, Israel Tel Aviv Sourasky Medical Center Tel Aviv, Israel, 64239 Italy Istituto Clinico Humanitas Rozzano, MI, Italy, 20089 AOU S. Orsola Malpighi Bologna Bologna, Italy, 40138 Fondazione IRCCS Cà Granda Ospedale Maggiore Policlinico Milano, Italy, 20122 Azienda Ospedaliera Universitaria Policlinico di Modena Modena, Italy, 41124 A.O.U. Federico II Napoli, Italy, 80131 A.O. U. Policlinico Paolo Giaccone Palermo, Italy, 90127 收起 <<
NCT01011439	Thymic Carcinoma	Phase 2	Active, not recruiting	December 2018	United States, Arizona ... 展开 >> TGen Clinical Research Services at Scottsdale Healthcare Scottsdale, Arizona, United States, 85258 United States, Maryland NIH, Center for Cancer Research, Medical Oncology Bethesda, Maryland, United States, 20892 France Hopital Larrey Toulouse Cedex, France, 31059 Institut de cancerologie Gustave Roussy Villejuif Cedex, France, 94805 Italy Fondazione IRCCS Istituto Nazionale dei Tumori di Milano Milano, (mi), Italy, 20133 Azienda Ospedaliera San Luigi Gonzaga Orbassano, Italy, 10043 收起 <<
NCT01301391	-		Active, not recruiting	-	-

Milciclib 参考文献

[1]Caporali S, Alvino E, et al. The cyclin-dependent kinase inhibitor PHA-848125 suppresses the in vitro growth of human melanomas sensitive or resistant to temozolomide, and shows synergistic effects in combination with this triazene compound. Pharmacol Res. 2010 May;61(5):437-48.

[2]Brasca MG, Amboldi N, et al. Identification of N,1,4,4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl] amino}-4,5-dihydro-1H-py razolo[4,3-h] quinazoline-3-carboxamide (PHA-848125), a potent, orally available cyclin dependent kinase inhibitor. J Med Chem. 2009 Aug 27;52(16):5152-63.

[3]Misra RN, Xiao Hy, Rawlins DB, Shan W, Kellar KA, Mulheron JG, Sack JS, Tokarski JS, Kimball SD, Webster KR. 1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases: highly potent 2,6-Difluorophenacyl analogues. Bioorg Med Chem Lett. 2003 Jul 21;13(14):2405-8. doi: 10.1016/s0960-894x(03)00381-0. PMID: 12824044.

[4]Caporali S, Alvino E, Levati L, Esposito AI, Ciomei M, Brasca MG, Del Bufalo D, Desideri M, Bonmassar E, Pfeffer U, D'Atri S. Down-regulation of the PTTG1 proto-oncogene contributes to the melanoma suppressive effects of the cyclin-dependent kinase inhibitor PHA-848125. Biochem Pharmacol. 2012 Sep 1;84(5):598-611. doi: 10.1016/j.bcp.2012.06.004. Epub 2012 Jun 13. PMID: 22704958.

[5]Albanese C, Alzani R, Amboldi N, Avanzi N, Ballinari D, Brasca MG, Festuccia C, Fiorentini F, Locatelli G, Pastori W, Patton V, Roletto F, Colotta F, Galvani A, Isacchi A, Moll J, Pesenti E, Mercurio C, Ciomei M. Dual targeting of CDK and tropomyosin receptor kinase families by the oral inhibitor PHA-848125, an agent with broad-spectrum antitumor efficacy. Mol Cancer Ther. 2010 Aug;9(8):2243-54. doi: 10.1158/1535-7163.MCT-10-0190. Epub 2010 Aug 3. PMID: 20682657.

Milciclib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.17mL

0.43mL

0.22mL

10.86mL

2.17mL

1.09mL

21.71mL

4.34mL

2.17mL

Milciclib 技术信息

CAS号	802539-81-7
分子式	C₂₅H₃₂N₈O
分子量	460.575

别名	PHA-848125
运输	蓝冰

存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place,Sealed in dry,Store in freezer, under -20°C

溶解度

DMSO: 18 mg/mL(39.08 mM)，配合低频超声助溶，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

30% propylene glycol+5% Tween 80+65% water 30 mg/mL suspension

Milciclib {[allProObj[0].p_purity_real_show]}

Milciclib 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Milciclib 质控信息

Milciclib 生物活性

Milciclib 细胞研究

Milciclib 临床研究

Milciclib 参考文献

Milciclib 实验方案

Milciclib 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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CDK5	CDK5/p35, IC50:265 nM
CDK4	CDK4/CyclinD1, IC50:160 nM
CDK2	CDK2/CyclinE, IC50:363 nM CDK2/CyclinA, IC50:45 nM
CDK7	CDK7/CyclinH, IC50:150 nM
CDK1	CDK1/CyclinB, IC50:398 nM

Milciclib {[allProObj[0].p_purity_real_show]}

Milciclib 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Milciclib 质控信息

Milciclib 生物活性

Milciclib 细胞研究

Milciclib 临床研究

Milciclib 参考文献

Milciclib 实验方案

Milciclib 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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Milciclib 纯度/质量文件产品仅供科研