WHI-P154 | JAK3 Inhibitor II | EGFR Inhibitor | AmBeed-信号通路专用抑制剂

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WHI-P154 98%

货号：A134082 同义名： JAK3 Inhibitor II;Janus-Associated Kinase 3 Inhibitor II

WHI-P154 is a specific inhibitor of JAK3 with IC50 value of 1.8 μM, almost shows no activity against JAK1 or JAK2.

WHI-P154 化学结构
CAS号：211555-04-3

WHI-P154 3D分子结构
CAS号：211555-04-3

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WHI-P154 纯度/质量文件产品仅供科研

货号：A134082 标准纯度： 98% 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
VEGFR 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, IC50: 3 nM JAK2 (V617F), 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		VEGFR,EGFR,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, 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。

产品名称	VEGFR1 ↓ ↑	VEGFR2 ↓ ↑	VEGFR3 ↓ ↑	其他靶点	纯度
Motesanib Diphosphate	++++ VEGFR1, IC50: 2 nM	++++ VEGFR2, IC50: 3 nM VEGFR2/Flk1, IC50: 3 nM	+++ VEGFR3, IC50: 6 nM	RET,PDGFR	98%
Tivozanib	++ VEGFR1, IC50: 30 nM	+++ VEGFR2, IC50: 6.5 nM	++ VEGFR3, IC50: 15 nM		99%+
Brivanib	+ VEGFR1, IC50: 380 nM	++ Flk1, IC50: 25 nM VEGFR2, IC50: 25 nM			99%+
Regorafenib	+++ VEGFR1, IC50: 13 nM	+++ VEGFR2, IC50: 4.2 nM	+ VEGFR3, IC50: 46 nM	RET	98%
Pazopanib	+++ VEGFR1, IC50: 10 nM	++ VEGFR2, IC50: 30 nM	+ VEGFR3, IC50: 47 nM	FGFR,PDGFR,c-Kit	99%
Sitravatinib	+++ VEGFR1 (FLT1), IC50: 6 nM	+++ VEGFR2 (KDR), IC50: 5 nM	++++ VEGFR3 (FLT4), IC50: 2 nM		99%+
Foretinib	+++ VEGFR1/FLT1, IC50: 6.8 nM	++++ KDR, IC50: 0.86 nM	++++ VEGFR3/FLT4, IC50: 2.8 nM	Tie-2	99%+
MGCD-265 analog	++++ VEGFR1, IC50: 3 nM	++++ VEGFR2, IC50: 3 nM	++++ VEGFR3, IC50: 4 nM	Tie-2	99%+
Lactate	+++ VEGFR1/FLT1, IC50: 10 nM	+++ VEGFR2/Flk1, IC50: 13 nM	+++ VEGFR3/FLT4, IC50: 8 nM	FLT3,c-Kit	85%
AEE788	+ FLT1, IC50: 59 nM	+ KDR, IC50: 77 nM		EGFR	98+%
Linifanib	++++ VEGFR1/FLT1, IC50: 3 nM	++++ VEGFR2/KDR, IC50: 4 nM	+ VEGFR3/FLT4, IC50: 190 nM	FLT3	99%+
Vatalanib 2HCl	+ VEGFR1/FLT1, IC50: 77 nM	++ VEGFR2/KDR, IC50: 37 nM VEGFR2/Flk1, IC50: 270 nM	+ VEGFR3/FLT4, IC50: 660 nM	c-Fms,c-Kit	99%+
Axitinib	++++ VEGFR1/FLT1, IC50: 0.1 nM	++++ VEGFR2/KDR, IC50: 0.2 nM VEGFR2/Flk1, IC50: 0.18 nM			98%
Dovitinib	+++ VEGFR1/FLT1, IC50: 10 nM	+++ VEGFR2/Flk1, IC50: 13 nM	+++ VEGFR3/FLT4, IC50: 8 nM	FLT3,c-Kit	99%+
ZM 306416	+ VEGFR1, IC50: 0.33 μM			Src	99%+
KRN-633	+ VEGFR1, IC50: 170 nM	+ VEGFR2, IC50: 160 nM	+ VEGFR3, IC50: 125 nM	c-Kit,BTK	98%
OSI-930	+++ FLT1, IC50: 8 nM	+++ KDR, IC50: 9 nM			99%+
Lenvatinib	++ VEGFR1/FLT1, IC50: 22 nM	++++ VEGFR2/KDR, IC50: 4.0 nM	+++ VEGFR3/FLT4, IC50: 5.2 nM		98%
NVP-BAW2881	+ hVEGFR1, IC50: 820 nM	+++ hVEGFR2, IC50: 9 nM mVEGF2, IC50: 165 nM	+ hVEGFR3, IC50: 420 nM		98%
Cediranib	+++ VEGFR1/FLT1, IC50: 5 nM	++++ VEGFR2/KDR, IC50: 0.5 nM		c-Kit	99%+
Nintedanib	++ VEGFR1, IC50: 34 nM	+++ VEGFR2, IC50: 13 nM	+++ VEGFR3, IC50: 13 nM	FLT3	99+%
BMS-794833		++ VEGFR2, IC50: 15 nM			99%+
SKLB1002		++ VEGFR2, IC50: 32 nM			98%
Cabozantinib S-malate		++++ VEGFR2/KDR, IC50: 0.035 nM			99+%
Ki8751		++++ VEGFR2, IC50: 0.9 nM		c-Kit	98+%
SU 5402		++ VEGFR2, IC50: 20 nM			98%
Rivoceranib Mesylate		++++ VEGFR2, IC50: 1 nM		RET	98+%
Ponatinib		++++ VEGFR2, IC50: 1.5 nM			98%
LY2874455		+++ VEGFR2, IC50: 7 nM			99%+
ZM323881 HCl		++++ VEGFR2, IC50: <2 nM			98%
AZD2932		+++ VEGFR-2, IC50: 8 nM		c-Kit	98%
Cabozantinib		++++ VEGFR2/KDR, IC50: 0.035 nM			98%
Sorafenib		++ VEGFR2, IC50: 90 nM VEGFR2/Flk1, IC50: 90 nM			99%
CYC-116		++ VEGFR2, Ki: 44 nM		FLT3	99%+
Golvatinib		++ VEGFR2, IC50: 16 nM			99%+
Sunitinib		+ VEGFR2 , IC50: 80 nM		FLT3	98%
RAF265		++ VEGFR2, EC50: 30 nM			99%+
PD173074					99%+
BFH772		++++ VEGFR2, IC50: 3 nM			98%
Semaxinib		+ VEGFR2/Flk1, IC50: 1.23 μM			98%
Vandetanib		++ VEGFR2, IC50: 40 nM	+ VEGFR3, IC50: 110 nM	EGFR	98%
SAR131675			++ VEGFR3, IC50: 23 nM		99%+
ENMD-2076		+ VEGFR2/KDR, IC50: 58.2 nM	++ VEGFR3/FLT4, IC50: 15.9 nM	RET,FLT3	98%
Telatinib		+++ VEGFR2, IC50: 6 nM	++++ VEGFR3, IC50: 4 nM	c-Kit	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。

WHI-P154 生物活性

靶点

JAK3

JAK3, IC50:1.8 μM
EGFR/ErbB1

EGFR, IC50:4 nM

描述

WHI-P154 is a potent inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase with an IC50 value of 4nM. It also has modest activity against Janus kinase 3 (JAK3) with an IC50 value of 1.8μM^[3]. WHI-P154 at 1 and 4μM significantly enhanced the cytotoxic effects of mitoxantrone and SN-38 in ABCG2-transfected cells but not in HEK293/pcDNA3.1 cells. Treatment of parental KB-3-1 cells and ABCB1-overexpressing KB-C2 cells with 4μM WHI-P154 resulted in moderate inhibition on ABCB1. The exposure of WHI-P154 (1 and 4μM) and 2.5μM FTC significantly increased the intracellular level of [³H]-mitoxantrone in ABCG2-overexpressing cells. Treatment of ABCG2-482-R2 cells with 4μM WHI-P154 blocked the efflux function of ABCG2^[4]. In mice bearing H694R or E1384K tumors, intravenous injection of WHI-P154 (1mg/kg per day) for 5 weeks significantly suppressed tumor growth and decreased phospho-Y1604 ALK expression in xenografted tumors when compared with DMSO-treated controls^[5].

WHI-P154 参考文献

[1]Changelian PS, Moshinsky D, et al. The specificity of JAK3 kinase inhibitors. Blood. 2008 Feb 15;111(4):2155-7.

[2]Sareila O, Korhonen R, et al. JAK inhibitors AG-490 and WHI-P154 decrease IFN-gamma-induced iNOS expression and NO production in macrophages. Mediators Inflamm. 2006;2006(2):16161.

[3]Changelian PS, Moshinsky D, Kuhn CF, et al. The specificity of JAK3 kinase inhibitors [published correction appears in Blood. 2009 Oct 1;114(14):3132. Dosage error in article text; Whipple, David A [added]]. Blood. 2008;111(4):2155-2157. doi:10.1182/blood-2007-09-115030

[4]Zhang H, Zhang YK, Wang YJ, et al. WHI-P154 enhances the chemotherapeutic effect of anticancer agents in ABCG2-overexpressing cells. Cancer Sci. 2014;105(8):1071-1078. doi:10.1111/cas.12462

[5]Wang YW, Tu PH, Lin KT, Lin SC, Ko JY, Jou YS. Identification of oncogenic point mutations and hyperphosphorylation of anaplastic lymphoma kinase in lung cancer. Neoplasia. 2011;13(8):704-715. doi:10.1593/neo.11222

WHI-P154 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.66mL

0.53mL

0.27mL

13.29mL

2.66mL

1.33mL

26.58mL

5.32mL

2.66mL

WHI-P154 技术信息

CAS号	211555-04-3
分子式	C₁₆H₁₄BrN₃O₃
分子量	376.205

别名	JAK3 Inhibitor II;Janus-Associated Kinase 3 Inhibitor II;Janex1.
运输	蓝冰

存储条件

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 50 mg/mL(132.91 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 10 mg/mL clear

PO 0.5% CMC-Na 47 mg/mL suspension

WHI-P154 98%

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JAK3	JAK3, IC50:1.8 μM
EGFR/ErbB1	EGFR, IC50:4 nM

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