Gandotinib | LY2784544 | JAK Inhibitor | AmBeed-信号通路专用抑制剂

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Gandotinib 99%+

货号：A315267 同义名： LY2784544

Gandotinib (LY2784544) 是一种强效的 JAK2 抑制剂，其 IC50 为 3 nM。Gandotinib (LY2784544) 还抑制 FLT3、FLT4、FGFR2、TYK2 和 TRKB，其 IC50 值分别为 4 nM、25 nM、32 nM、44 nM 和 95 nM。

Gandotinib 化学结构
CAS号：1229236-86-5

Gandotinib 3D分子结构
CAS号：1229236-86-5

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Gandotinib 纯度/质量文件产品仅供科研

货号：A315267 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 >

JAK 亚型比较

产品名称	JAK1 ↓ ↑	JAK2 ↓ ↑	JAK3 ↓ ↑	Tyk2 ↓ ↑	其他靶点	纯度
Decernotinib	+++ JAK1, IC50: 11 nM JAK1, Ki: 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 (V617F), Ki: 0.245 nM JAK2, IC50: 0.288 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			RET,FLT3	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,VEGFR,Src	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		RET,FLT3	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。

Gandotinib 生物活性

靶点	JAK1 JAK1, IC50:19.8 nM JAK3 JAK3, IC50:48.0 nM Tyk2 TYK2, IC50:44 nM JAK2 JAK2 (V617F), Ki:0.245 nM JAK2, IC50:0.288 nM
描述	The JAK/STAT3 pathway is activated by various cancer types, including glioma, and blockade of the pathway induces cell death in cancer cells. The Janus family kinases (JAKs), JAK1, JAK2, JAK3, and TYK2, are involved in cell growth, survival, development, and differentiation of a variety of cells, particularly immune cells and hematopoietic cells. LY2784544 is a potent, selective and ATP-competitive inhibitor of janus kinase 2 (JAK2) tyrosine kinase with IC₅₀ of 3 nM. Gandotinib (LY2784544) also inhibits FLT3, FLT4, FGFR2, TYK2, and TRKB with IC₅₀ of 4, 25, 32, 44, and 95 nM, respectively and shows increased potency for the JAK2 _V617F mutation. LY2784544 effectively inhibited JAK2 _V617F -driven signaling and cell proliferation in Ba/F3 cells with IC₅₀ of 20 and 55 nM, respectively. In comparison, LY2784544 was much less potent at inhibiting interleukin-3-stimulated wild-type JAK2-mediated signaling and cell proliferation with IC₅₀ of 1183 and 1309 nM, respectively. In a mouse ascitic tumor model with Ba/F3-JAK2 _V617F-GFP cells, LY2784544 was administered once by oral gavage at a dose of 2.5, 5.0, 10.0, 20.0, 40.0, or 80.0 mg/kg to severe combined immunodeficiency mice to measure the inhibition of STAT5 phosphorylation. The result demonstrated that LY2784544 possess good inhibiting effect at STAT5 phosphorylation at indicated concentrations. LY2784544 also potently inhibited STAT5 phosphorylation in Ba/F3 cells expressing JAK2_V617F across a concentration range from 50 nM–20 μM^[3]. LY2784544 discovered in a focused screen at low micromolar concentrations, prevented Tf endocytosis as well as trypanosome proliferation with GI50 1.0-3.1 μM^[4].
作用机制	LY2784544 targets the adenosine triphosphate (ATP) binding site at the TK domain, thus affecting both mutated and wild-type kinases.

Gandotinib 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
NCT01134120	Myeloproliferative Disorders ... 展开 >> Thrombocythemia, Essential Polycythemia Vera Primary Myelofibrosis 收起 <<	Phase 1	Completed	-	United States, Texas ... 展开 >> For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Houston, Texas, United States, 77030 United States, Utah For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Salt Lake City, Utah, United States, 84132 收起 <<
NCT01577355	Healthy Male Volunteers	Phase 1	Completed	-	United States, Wisconsin ... 展开 >> For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Madison, Wisconsin, United States, 53704 收起 <<
NCT01594723	Neoplasms, Hematologic	Phase 2	Active, not recruiting	December 31, 2019	-

Gandotinib 参考文献

[1]Douglas JJ, Cole KP, Stephenson CR. Photoredox catalysis in a complex pharmaceutical setting: toward the preparation of JAK2 inhibitor LY2784544. J Org Chem. 2014 Dec 5;79(23):11631-43.

[2]Ma L, Clayton JR, et al. Discovery and characterization of LY2784544, a small-molecule tyrosine kinase inhibitor of JAK2V617F. Blood Cancer J. 2013 Apr 12;3:e109.

[3]Ma L, Clayton JR, Walgren RA, Zhao B, Evans RJ, Smith MC, Heinz-Taheny KM, Kreklau EL, Bloem L, Pitou C, Shen W, Strelow JM, Halstead C, Rempala ME, Parthasarathy S, Gillig JR, Heinz LJ, Pei H, Wang Y, Stancato LF, Dowless MS, Iversen PW, Burkholder TP. Discovery and characterization of LY2784544, a small-molecule tyrosine kinase inhibitor of JAK2V617F. Blood Cancer J. 2013 Apr 12;3(4):e109. doi: 10.1038/bcj.2013.6. PMID: 23584399; PMCID: PMC3641321.}

[4]Santos FP, Verstovsek S. JAK2 inhibitors for myelofibrosis: why are they effective in patients with and without JAK2V617F mutation? Anticancer Agents Med Chem. 2012 Nov;12(9):1098-109. doi: 10.2174/187152012803529727. PMID: 22583424.

Gandotinib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.13mL

0.43mL

0.21mL

10.64mL

2.13mL

1.06mL

21.28mL

4.26mL

2.13mL

Gandotinib 技术信息

CAS号	1229236-86-5
分子式	C₂₃H₂₅ClFN₇O
分子量	469.942

别名	LY2784544
运输	蓝冰

存储条件

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 50 mg/mL(106.4 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

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

NCT01134120	Myeloproliferative Disorders ... 展开 >> Thrombocythemia, Essential Polycythemia Vera Primary Myelofibrosis 收起 <<	Phase 1	Completed	-	United States, Texas ... 展开 >> For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Houston, Texas, United States, 77030 United States, Utah For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Salt Lake City, Utah, United States, 84132 收起 <<
NCT01577355	Healthy Male Volunteers	Phase 1	Completed	-	United States, Wisconsin ... 展开 >> For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Madison, Wisconsin, United States, 53704 收起 <<
NCT01594723	Neoplasms, Hematologic	Phase 2	Active, not recruiting	December 31, 2019	-
NCT01520220	Myeloproliferative Neoplasms o... 展开 >>f Polycythemia Vera Essential Thrombocythemia Myelofibrosis 收起 <<	Phase 1	Completed	-	United States, Alabama ... 展开 >> For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Birmingham, Alabama, United States, 35249 United States, Arizona For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Scottsdale, Arizona, United States, 85259 United States, Arkansas For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Fayetteville, Arkansas, United States, 72703 United States, District of Columbia For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Washington, District of Columbia, United States, 20007 United States, Florida For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Jacksonville, Florida, United States, 32224 United States, Hawaii For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Honolulu, Hawaii, United States, 96813 United States, South Carolina For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Charleston, South Carolina, United States, 29425 United States, Utah For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Salt Lake City, Utah, United States, 84132 United States, Wisconsin For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Milwaukee, Wisconsin, United States, 53226 收起 <<

Gandotinib 99%+

Gandotinib 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Gandotinib 质控信息

Gandotinib 生物活性

Gandotinib 临床研究

Gandotinib 参考文献

Gandotinib 实验方案

Gandotinib 技术信息

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JAK1	JAK1, IC50:19.8 nM
JAK3	JAK3, IC50:48.0 nM
Tyk2	TYK2, IC50:44 nM
JAK2	JAK2 (V617F), Ki:0.245 nM JAK2, IC50:0.288 nM

Gandotinib 99%+

Gandotinib 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Gandotinib 质控信息

Gandotinib 生物活性

Gandotinib 临床研究

Gandotinib 参考文献

Gandotinib 实验方案

Gandotinib 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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Gandotinib 纯度/质量文件产品仅供科研