Momelotinib | CYT387 | JAK1/2 Inhibitor | AmBeed-信号通路专用抑制剂

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Momelotinib {[allProObj[0].p_purity_real_show]}

货号：A207449 同义名： CYT387;LM-1149

Momelotinib（CYT387）是一种ATP竞争性JAK1/JAK2抑制剂，其IC50值分别为11 nM和18 nM，对JAK3的活性显著较低。

Momelotinib 化学结构
CAS号：1056634-68-4

Momelotinib 3D分子结构
CAS号：1056634-68-4

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Momelotinib 纯度/质量文件产品仅供科研

货号：A207449 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: • Cell, 2024, 101755. Ambeed. [ A399663 ]; • EMBO J., 2024. Ambeed. [ A295334 ]; • JMC, 2024, 67(20): 18265-18289. Ambeed. [ A538667 , A341145 , A117430 , A172297 ]; • JMC, 2024. Ambeed. [ A210558 , A1518164 ]; • Cell Death Discov., 2024, 10, 436. Ambeed. [ A384235 ]; 更多 >

JAK 亚型比较

产品名称	JAK1 ↓ ↑	JAK2 ↓ ↑	JAK3 ↓ ↑	Tyk2 ↓ ↑	其他靶点	纯度
Decernotinib	+++ JAK1, Ki: 11 nM JAK1, IC50: 11 nM	+++ JAK2, Ki: 13 nM	++++ JAK3, Ki: 2.5 nM	+++ TYK2, Ki: 13 nM		99%+
ZM39923 HCl	+ JAK1, pIC50: 4.4		+ JAK3, pIC50: 7.1		EGFR	97%
Cerdulatinib	+++ JAK1, IC50: 12 nM	+++ JAK2, IC50: 6 nM	+++ JAK3, IC50: 8 nM	++++ TYK2, IC50: 0.5 nM		99%+
Momelotinib	+++ JAK1, IC50: 11 nM	++ JAK2, IC50: 18 nM	+ JAK3, IC50: 155 nM			99%+
XL019	+ JAK1, IC50: 134.3 nM	++++ JAK2, IC50: 2.2 nM	+ JAK3, IC50: 214.2 nM		FLT3	99%+
Ruxolitinib	+++ JAK1, IC50: 3.3 nM	++++ JAK2, IC50: 2.8 nM				98%
Tofacitinib	+ JAK1, IC50: 112 nM	++ JAK2, IC50: 20 nM	++++ JAK3, IC50: 1 nM			98%
Ruxolitinib (S enantiomer)	+++ JAK1, IC50: 3.3 nM	++++ JAK2, IC50: 2.8 nM		++ TYK2, IC50: 19 nM		98%
Filgotinib	+++ JAK1, IC50: 10 nM	++ JAK2, IC50: 28 nM	+ JAK3, IC50: 810 nM	+ TYK2, IC50: 116 nM		99%
Baricitinib	+++ JAK1, IC50: 5.9 nM	+++ JAK2, IC50: 5.7 nM		++ TYK2, IC50: 53 nM		99%
Gandotinib	++ JAK1, IC50: 19.8 nM	++++ JAK2, IC50: 0.288 nM JAK2 (V617F), Ki: 0.245 nM	++ JAK3, IC50: 48.0 nM	++ TYK2, IC50: 44 nM	FLT3	99%+
Oclacitinib maleate	+++ JAK1, IC50: 10nM	++ JAK2, IC50: 18nM	+ JAK3, IC50: 99nM	+ TYK2, IC50: 84nM		98+%
NVP-BSK805 2HCl	++ JAK1, IC50: 31.63 nM	++++ JAK2, IC50: ~0.5 nM	++ JAK3, IC50: 18.68 nM	+++ TYK2, IC50: 10.76 nM		99+%
Peficitinib		✔				98%
Go6976		✔			FLT3	99%+
AZD-1480		++++ JAK2, IC50: 0.26 nM				99%+
Fedratinib		+++ JAK2 (V617F), IC50: 3 nM JAK2, IC50: 3 nM			FLT3,RET	99%+
WP1066		+ JAK2, IC50: 2.3 μM				98%
Curcumol		✔				98%
AZ960		++++ JAK2, Ki: 0.45 nM JAK2, IC50: <3 nM				97%
GLPG0634 analog		✔				99%+
CEP-33779		++++ JAK2, IC50: 1.8 nM				99%+
FLLL32		+ JAK2, IC50: <5 μM				99%+
WHI-P154			+ JAK3, IC50: 1.8 μM		EGFR,Src,VEGFR	98%
BMS-911543		++++ JAK2, IC50: 1.1 nM	+ JAK3, IC50: 75 nM	++ TYK2, IC50: 66 nM		98%
TG101209		+++ JAK2, IC50: 6 nM	+ JAK3, IC50: 169 nM		FLT3,RET	99%+
AT9283		++++ JAK2, IC50: 1.2 nM	++++ JAK3, IC50: 1.1 nM			99%+
Pacritinib		++ JAK2 (V617F), IC50: 19 nM JAK2, IC50: 23 nM	+ JAK3, IC50: 520 nM	++ TYK2, IC50: 50 nM	FLT3	97%
Tofacitinib citrate		++ JAK2, IC50: 20 nM	++++ JAK3, IC50: 1 nM			99%
FM-381			++++ JAK3, IC50: 127 pM			98%
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。

Momelotinib 生物活性

靶点

JAK1

JAK1, IC50:11 nM
JAK3

JAK3, IC50:155 nM
JAK2

JAK2, IC50:18 nM

描述

CYT387 (Momelotinib) is an ATP-competitive inhibitor of JAK1 and JAK2 with IC50s of 11 nM and 18 nM while less activity against other kinases including JAK3 (IC50 = 155 nM). MECNISIM. CYT387 inhibits proliferation of JAK2V617F mutation HEL cells as well as Ba/F3-wt and Ba/F3-JAK2V67F cells with IC50 of approximately 1400~1500 nM. Proliferation of Ba/F3-MPLW515L cell was also inhibited with IC50 = 200 nM. In human erythroleukemia (HEL) cells, CYT387 inhibits phosphorylation of STAT-5 and STAT-3 with IC50s of 400 nM and 2500 nM. Besides, CYT387 can also inhibit in vitro erythroid colony formation in polycythemia vera patients.[1]Together with paclitaxel, CYT387-treated human ovarian HEY cells showed a significant reduced tumor burden compared to that with paclitaxel only-treated transplanted cells in mice.[2] CYT387 could be used in the treatment of primary myelofibrosis or post-polycythemia vera or post-essential thrombocythemia myelofibrosis (post-PV/ET MF), as well as the treatment for relapsed or refractory metastatic pancreatic ductal adenocarcinoma (in combination with capecitabine and oxaliplatin).

Momelotinib 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 HEL 92.1.7 cells		Proliferation assay	72 h	Antiproliferative activity against human HEL 92.1.7 cells expressing JAK2 V617F mutant kinase after 72 hrs by alamar blue assay, IC50=1.804 μM	19762238
human SET2 cells		Proliferation assay	72 h	Antiproliferative activity against human SET2 cells expressing JAK2 V617F mutant kinase after 72 hrs by alamar blue assay, IC50=0.232 μM	19762238
mouse BAF3 cells		Proliferation assay	72 h	Antiproliferative activity against mouse BAF3 cells expressing TEL-JAK2 kinase after 72 hrs by alamar blue assay	19762238

Momelotinib 动物研究

Dose	Mice: 25 mg/kg, 50 mg/kg^[3] (p.o.), 100 mg/kg^[4] (p.o.)
Administration	p.o.

Momelotinib 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
NCT02251821	Primary Myelofibrosis ... 展开 >> Secondary Myelofibrosis 收起 <<	Phase 2	Recruiting	-	United States, Washington ... 展开 >> Fred Hutch/University of Washington Cancer Consortium Recruiting Seattle, Washington, United States, 98109 Contact: Rachel B. Salit 206-667-1317 rsalit@fredhutch.org Principal Investigator: Rachel B. Salit 收起 <<
NCT02206763	EGFR Mutated EGFR TKI Naive Me... 展开 >>tastatic NSCLC 收起 <<	Phase 1	Terminated	-	United States, California ... 展开 >> Duarte, California, United States Palo Alto, California, United States Whittier, California, United States 收起 <<
NCT01998828	Polycythemia Vera ... 展开 >> Essential Thrombocythemia 收起 <<	Phase 2	Terminated	-	United States, Arizona ... 展开 >> Scottsdale, Arizona, United States United States, California Whittier, California, United States United States, Mississippi Tupelo, Mississippi, United States United States, Missouri Saint Louis, Missouri, United States United States, Texas Houston, Texas, United States Australia, Victoria Frankston, Victoria, Australia Parkville, Victoria, Australia Canada, Ontario Toronto, Ontario, Canada Canada, Quebec Montreal, Quebec, Canada Canada Vancouver, Canada France La Tronche, France Nantes Cedex 1, France Paris, France Germany Dresden, Germany Minden, Germany 收起 <<

Momelotinib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.41mL

0.48mL

0.24mL

12.06mL

2.41mL

1.21mL

24.13mL

4.83mL

2.41mL

Momelotinib 技术信息

CAS号	1056634-68-4
分子式	C₂₃H₂₂N₆O₂
分子量	414.46

别名	CYT387;LM-1149 ;CYT11387
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,2-8°C

溶解度

DMSO: 9 mg/mL(21.72 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

IP 2% DMSO+2% Tween80+40% PEG300+water 6 mg/mL clear

PO 0.5% CMC-Na 35 mg/mL suspension

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

NCT02251821	Primary Myelofibrosis ... 展开 >> Secondary Myelofibrosis 收起 <<	Phase 2	Recruiting	-	United States, Washington ... 展开 >> Fred Hutch/University of Washington Cancer Consortium Recruiting Seattle, Washington, United States, 98109 Contact: Rachel B. Salit 206-667-1317 rsalit@fredhutch.org Principal Investigator: Rachel B. Salit 收起 <<
NCT02206763	EGFR Mutated EGFR TKI Naive Me... 展开 >>tastatic NSCLC 收起 <<	Phase 1	Terminated	-	United States, California ... 展开 >> Duarte, California, United States Palo Alto, California, United States Whittier, California, United States 收起 <<
NCT01998828	Polycythemia Vera ... 展开 >> Essential Thrombocythemia 收起 <<	Phase 2	Terminated	-	United States, Arizona ... 展开 >> Scottsdale, Arizona, United States United States, California Whittier, California, United States United States, Mississippi Tupelo, Mississippi, United States United States, Missouri Saint Louis, Missouri, United States United States, Texas Houston, Texas, United States Australia, Victoria Frankston, Victoria, Australia Parkville, Victoria, Australia Canada, Ontario Toronto, Ontario, Canada Canada, Quebec Montreal, Quebec, Canada Canada Vancouver, Canada France La Tronche, France Nantes Cedex 1, France Paris, France Germany Dresden, Germany Minden, Germany 收起 <<
NCT01969838	Primary Myelofibrosis ... 展开 >> Post-Polycythemia Vera Myelofibrosis Post-Essential Thrombocythemia Myelofibrosis 收起 <<	Phase 3	Active, not recruiting	March 2019	-
NCT02101021	Metastatic Pancreatic Ductal A... 展开 >>denocarcinoma 收起 <<	Phase 3	Terminated	-	United States, California ... 展开 >> Cedars-Sinai Medical Center Los Angeles, California, United States, 90048 United States, Indiana Indiana University Health Goshen Center for Cancer Care Goshen, Indiana, United States, 46506 United States, Massachusetts Dana Farber Cancer Institute Boston, Massachusetts, United States, 02215 United States, Washington Northwest Medical Specialties, PLLC Tacoma, Washington, United States, 98405 收起 <<
NCT02101268	Primary Myelofibrosis (PMF) ... 展开 >> Post-polycythemia Vera (Post-PV) Post-essential Thrombocythemia Myelofibrosis (Post-ET MF) 收起 <<	Phase 3	Active, not recruiting	March 2019	-
NCT02101021	-		Terminated	-	-
NCT02515630	Primary Myelofibrosis (PMF) ... 展开 >> Post-polycythemia Vera (Post-PV) Myelofibrosis Postessential Thrombocythemia (Post-ET) Myelofibrosis 收起 <<	Phase 2	Completed	-	United States, Arizona ... 展开 >> Phoenix, Arizona, United States United States, California Los Angeles, California, United States Orange, California, United States United States, Florida Jacksonville, Florida, United States United States, Maryland Baltimore, Maryland, United States United States, Michigan Ann Arbor, Michigan, United States United States, Missouri Saint Louis, Missouri, United States United States, New York Bronx, New York, United States New York, New York, United States United States, North Carolina Durham, North Carolina, United States United States, Ohio Cleveland, Ohio, United States United States, Texas Houston, Texas, United States Canada, Ontario Toronto, Ontario, Canada 收起 <<
NCT02258607	Relapsed Metastatic KRAS-Mutat... 展开 >>ed Non-Small Cell Lung Cancer 收起 <<	Phase 1	Terminated	-	United States, California ... 展开 >> Duarte, California, United States Sacramento, California, United States United States, Massachusetts Boston, Massachusetts, United States United States, Virginia Fairfax, Virginia, United States United States, Washington Spokane, Washington, United States 收起 <<
NCT01423058	Primary Myelofibrosis ... 展开 >> Post-Polycythemia Vera Post-Essential Thrombocythemia Myelofibrosis 收起 <<	Phase 1 Phase 2	Completed	-	United States, Arizona ... 展开 >> Mayo Clinic Scottsdale, Arizona, United States, 85259 United States, Florida Mayo Clinic Jacksonville, Florida, United States, 32224 United States, Texas MD Anderson Cancer Center, The University of Texas Houston, Texas, United States, 77030 United States, Utah Huntsman Cancer Institute at the University of Utah Salt Lake City, Utah, United States, 84108 Canada, Ontario Princess Margaret Hospital Toronto, Ontario, Canada, M5G 2M9 Canada, Quebec Jewish General Hospital Montreal, Quebec, Canada, H3T 1E2 收起 <<
NCT01236638	Primary Myelofibrosis ... 展开 >> Post-Polycythemia Vera Myelofibrosis Post-Essential Thrombocythemia Myelofibrosis 收起 <<	Phase 2	Completed	-	United States, California ... 展开 >> Stanford Cancer Center Stanford, California, United States, 94305-5821 United States, Massachusetts Dana-Farber Cancer Institute Boston, Massachusetts, United States, 02115 United States, Minnesota Mayo Clinic Rochester, Minnesota, United States, 55905 Australia, Victoria The Royal Melbourne Hospital Parkville, Victoria, Australia, 3050 Canada, Ontario Princess Margaret Hospital Toronto, Ontario, Canada, M5G 2M9 Canada, Quebec Jewish General Hospital Montreal, Quebec, Canada, H3T 1E2 收起 <<
NCT02124746	Primary Myelofibrosis ... 展开 >> Post-Polycythemia Vera Myelofibrosis Post-Essential Thrombocythemia Myelofibrosis Polycythemia Vera Essential Thrombocythemia 收起 <<	Phase 2	Completed	-	-
NCT02244489	Relapsed/Refractory Metastatic... 展开 >> Pancreatic Ductal Adenocarcinoma 收起 <<	Phase 1	Terminated	-	United States, Arizona ... 展开 >> Scottsdale Healthcare Research Institute Scottsdale, Arizona, United States, 85258 United States, California Cedars-Sinai Medical Center Los Angeles, California, United States, 90048 United States, Tennessee Tennessee Oncology Nashville, Tennessee, United States, 37203 United States, Virginia Virginia Cancer Specialists, PC Fairfax, Virginia, United States, 22031 收起 <<
NCT03441113	Post-polycythemia Vera Myelofi... 展开 >>brosis (Post-PV MF) Primary Myelofibrosis (PMF) Post-essential Thrombocythemia Myelofibrosis (Post-ET MF) 收起 <<	Phase 2	Enrolling by invitation	June 2020	-
NCT00935987	Primary Myelofibrosis ... 展开 >> Post-Polycythemia Vera Myelofibrosis Post-Essential Thrombocythemia Myelofibrosis 收起 <<	Phase 1 Phase 2	Completed	-	United States, California ... 展开 >> Stanford Cancer Center Stanford, California, United States, 94305-5821 United States, Massachusetts Dana-Farber Cancer Institute Boston, Massachusetts, United States, 02115 United States, Minnesota Mayo Clinic Rochester, Minnesota, United States, 55905 Australia, Victoria The Royal Melbourne Hospital Parkville, Victoria, Australia, 3050 Canada, Ontario Princess Margaret Hospital Toronto, Ontario, Canada, M5G 2M9 Canada, Quebec Jewish General Hospital Montreal, Quebec, Canada, H3T 1E2 收起 <<

Momelotinib {[allProObj[0].p_purity_real_show]}

Momelotinib 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Momelotinib 质控信息

Momelotinib 生物活性

Momelotinib 细胞研究

Momelotinib 动物研究

Momelotinib 临床研究

Momelotinib 实验方案

Momelotinib 技术信息

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JAK1	JAK1, IC50:11 nM
JAK3	JAK3, IC50:155 nM
JAK2	JAK2, IC50:18 nM

Momelotinib {[allProObj[0].p_purity_real_show]}

Momelotinib 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Momelotinib 质控信息

Momelotinib 生物活性

Momelotinib 细胞研究

Momelotinib 动物研究

Momelotinib 临床研究

Momelotinib 实验方案

Momelotinib 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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Momelotinib 纯度/质量文件产品仅供科研