BMS-911543 | JAK Inhibitor | AmBeed-信号通路专用抑制剂

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BMS-911543 {[allProObj[0].p_purity_real_show]}

货号：A287429

BMS-911543 is a selective ATP-competitive JAK2 inhibitor with IC50 value of 1.1 nM, with much less potency against JAK1, JAK3 and TYK2 with IC50 values of 360nM, 75 nM and 66nM.

BMS-911543 化学结构
CAS号：1271022-90-2

BMS-911543 3D分子结构
CAS号：1271022-90-2

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BMS-911543 纯度/质量文件产品仅供科研

货号：A287429 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

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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, 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, IC50: 3 nM JAK2 (V617F), IC50: 3 nM			FLT3,RET	99%+
WP1066		+ JAK2, IC50: 2.3 μM				98%
Curcumol		✔				98%
AZ960		++++ JAK2, IC50: <3 nM JAK2, Ki: 0.45 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, IC50: 23 nM JAK2 (V617F), IC50: 19 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。

BMS-911543 生物活性

靶点	JAK3 JAK3, IC50:75 nM Tyk2 TYK2, IC50:66 nM JAK2 JAK2, IC50:1.1 nM
描述	The Janus kinases (JAK) are a class of non-receptor tyrosine kinases essential for cytokine signal transduction via the JAK/STAT pathway. BMS-911543 is a potent, selective inhibitor of JAK2 with an IC50 value of 1.1 nM. The dissociation constant (K_i) values of BMS-911543 for JAK1, JAK2 and JAK3 are 1114, 0.48 and 357 nM, respectively. BMS-911543 displayed a dose-dependent anti-proliferative effect in JAK2^V617F-dependent cells such as SET2 and Ba/F3 with IC50 values of 60 and 70 nM, respectively. In Ba/F^JAK2V617F cells, BMS-911543 treatment resulted in dose-dependent reduction of pSTAT5 with an IC50 value of 60 nM. In human whole-blood ex vivo assay, BMS-911543 dose-dependently inhibited TPO-stimulated pSTAT5 in human platelets. In primary hematopoetic CD34⁺ progenitors isolated from normal healthy volunteers, BMS-911543 inhibited EPO-mediated burst forming unit-erythroid (BFU-E) colony growth with an IC50 of approximately 1.5 μM. In cells isolated from JAK2^V617F-positive MPN patient, BMS-911543 inhibited BFU-E with an IC50 of 0.3 μM in the presence of EPO compared with an IC50 of 0.075 μM in EPO-independent erythroid colony formation. A single oral dose of 30 mg/kg BMS-911543 in PD-PK mouse model fully inhibited pSTAT5 induction at 1 – 18h post treatment. In athymic mice xenografted with SET2 cells, 10 mg/kg BMS-911543 demonstrated 90 – 100% pSTAT5 inhibition up to 7h post dose. In a mouse model of antigen-induced antibody production, BMS-911543 at 10 and 30 mg/kg resulted in 65% and 85% reduction, respectively, in the level of IgG antibody^[4].
作用机制	BMS-911543 is a selective ATP-competitive inhibitor of JAK2^[4].

BMS-911543 动物研究

Dose

Mice: 3 mg/kg - 30 mg/kg^[3] (p.o.); 2 mg/kg^[1] (i.v.) Rat: 1 mg/kg^[1] (i.v./p.o.)

Administration

p.o., i.v.

Pharmacokinetics

Animal	Mice^[1]	Rats^[1]	Dogs^[1]	Monkeys^[1]
Dose	2.0 mg/kg (i.v.) 10 mg/kg (p.o.)	1.0 mg/kg (i.v.) 1.0 mg/kg (p.o.)	0.2 mg/kg (i.v.) 0.2 mg/kg (p.o.)	1.0 mg/kg (i.v.) 1.0 mg/kg (p.o.)
Administration	i.v. p.o.	i.v. p.o.	i.v. p.o.	i.v. p.o.
F	1	1	0.82	0.53
T_1/2	5.1 h	5 h	2.2 h	2.4 h
CL	0.55 ml/min/kg	0.7 ml/min/kg	6.5 ml/min/kg	5.3 ml/min/kg
Vss	0.26 L/kg	0.3 L/kg	1.6 L/kg	1.1 L/kg

BMS-911543 参考文献

[1]Wan H, Schroeder GM, et al. Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms. ACS Med Chem Lett. 2015 Jul 12;6(8):850-5.

[2]Purandare AV, McDevitt TM, et al. Characterization of BMS-911543, a functionally selective small-molecule inhibitor of JAK2. Leukemia. 2012 Feb;26(2):280-8.

[3]Pomicter AD, Eiring AM, et al. Limited efficacy of BMS-911543 in a murine model of Janus kinase 2 V617F myeloproliferative neoplasm. Exp Hematol. 2015 Jul;43(7):537-45.e1-11.

[4]Purandare AV, McDevitt TM, Wan H, You D, Penhallow B, Han X, Vuppugalla R, Zhang Y, Ruepp SU, Trainor GL, Lombardo L, Pedicord D, Gottardis MM, Ross-Macdonald P, de Silva H, Hosbach J, Emanuel SL, Blat Y, Fitzpatrick E, Taylor TL, McIntyre KW, Michaud E, Mulligan C, Lee FY, Woolfson A, Lasho TL, Pardanani A, Tefferi A, Lorenzi MV. Characterization of BMS-911543, a functionally selective small-molecule inhibitor of JAK2. Leukemia. 2012 Feb;26(2):280-8.

BMS-911543 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.31mL

0.46mL

0.23mL

11.56mL

2.31mL

1.16mL

23.12mL

4.62mL

2.31mL

BMS-911543 技术信息

CAS号	1271022-90-2
分子式	C₂₃H₂₈N₈O
分子量	432.521

别名
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: 25 mg/mL(57.8 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

BMS-911543 {[allProObj[0].p_purity_real_show]}

BMS-911543 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

BMS-911543 质控信息

BMS-911543 生物活性

BMS-911543 动物研究

BMS-911543 参考文献

BMS-911543 实验方案

BMS-911543 技术信息

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JAK3	JAK3, IC50:75 nM
Tyk2	TYK2, IC50:66 nM
JAK2	JAK2, IC50:1.1 nM

BMS-911543 {[allProObj[0].p_purity_real_show]}

BMS-911543 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

BMS-911543 质控信息

BMS-911543 生物活性

BMS-911543 动物研究

BMS-911543 参考文献

BMS-911543 实验方案

BMS-911543 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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BMS-911543 纯度/质量文件产品仅供科研