AZD-1480 | JAK1/2 Inhibitor | AmBeed-信号通路专用抑制剂

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AZD-1480 99%+

货号：A209618

AZD-1480 是一种 JAK1 和 JAK2 抑制剂，IC50 分别为 1.3 nM 和 0.4 nM。

AZD-1480 化学结构
CAS号：935666-88-9

AZD-1480 3D分子结构
CAS号：935666-88-9

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AZD-1480 纯度/质量文件产品仅供科研

货号：A209618 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, 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。

AZD-1480 生物活性

靶点

JAK2

JAK2, IC50:0.26 nM

描述

The signal transducer and activator of transcription (STAT) activation by cytokines is mediated through the Janus family kinases (Jak), which include four family members, Jak1, Jak2, Jak3, and Tyk2. JAK2 is a Non-receptor tyrosine kinase involved in various processes such as cell growth, development, differentiation or histone modifications. JAK2 mediates essential signaling events in both innate and adaptive immunity. Following ligand-binding to cell surface receptors, JAK2 phosphorylates specific tyrosine residues on the cytoplasmic tails of the receptor, creating docking sites for STATs proteins. AZD1480 is a potent ATP competitive inhibitor of JAK2 kinase, with an inhibition constant (Ki) of 0.26nM. The enzyme IC₅₀ of AZD1480 against JAK2, JAK1 and JAK3 were <0.4nM, 1.3nM and 3.9nM, respectively, at K_m ATP^[3]. In TEL-JAK2 cells, AZD1480 concentration-dependently inhibited the phosphorylation of Stat5 ranging from 0.03μM to 1μM, with an IC₅₀ of 46nM. Little or no inhibition of Stat5 phosphorylation was observed in the TEL-Jak3, TEL-Jak1, or TEL-Tyk2 cells at below 1μM AZD1480^[3]. At concentrations ranging from 0.5μM to 3μM, AZD1480 blocked cell proliferation and induces apoptosis of myeloma cell lines^[4]. In animal experiments, AZD1480 decreased tumor growth in Renca, Kms.11, TC32, Rh18 or patient derived Glioblastoma xenografts. In different experiments, AZD1480 was orally dosed 50mg/kg once a day or 30mg/kg, twice a day^[5].

AZD-1480 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
4C8	1 µM	Function Assay	0-16 h	inhibits constitutive STAT-3 and JAK2 activation	22027691
4C8	1/10 µM	Growth Inhibition Assay	24/48/72 h	inhibits cell proliferation at a concentration of 10 µM	22027691
686LN		Growth Inhibition Assay	72 h	EC50=2.05 ± 1.33 μM	25810010
8226	0.5-2 μM	Apoptosis Assay	48/72 h	induces apoptosis dose dependently	21164517

AZD-1480 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
NCT00910728	Primary Myelofibrosis (PMF) ... 展开 >> Post-Polycythaemia Vera Essential Thrombocythaemia Myelofibrosis 收起 <<	Phase 1	Completed	-	United States, New York ... 展开 >> Research Site New York, New York, United States United States, Texas Research Site Houston, Texas, United States France Research Site Villejuif Cedex, France 收起 <<
NCT01112397	Solid Malignancies	Phase 1	Terminated(Decision to stop de... 展开 >>velopment of AZD1480) 收起 <<	-	United States, Colorado ... 展开 >> Research Site Aurora, Colorado, United States United States, Michigan Research Site Detroit, Michigan, United States United States, Pennsylvania Research Site Philadelphia, Pennsylvania, United States 收起 <<
NCT00910728	-		Completed	-	-

AZD-1480 参考文献

[1]16(6):487-97.

[2]25(3):538-50.

[3]Hedvat M, Huszar D, Herrmann A, Gozgit JM, Schroeder A, Sheehy A, Buettner R, Proia D, Kowolik CM, Xin H, Armstrong B, Bebernitz G, Weng S, Wang L, Ye M, McEachern K, Chen H, Morosini D, Bell K, Alimzhanov M, Ioannidis S, McCoon P, Cao ZA, Yu H, Jove R, Zinda M. The JAK2 inhibitor AZD1480 potently blocks Stat3 signaling and oncogenesis in solid tumors. Cancer Cell. 2009 Dec 8;16(6):487-97.

AZD-1480 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.87mL

0.57mL

0.29mL

14.34mL

2.87mL

1.43mL

28.67mL

5.73mL

2.87mL

AZD-1480 技术信息

CAS号	935666-88-9
分子式	C₁₄H₁₄ClFN₈
分子量	348.766

别名
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(143.36 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+30% PEG300+water 2 mg/mL clear

PO 0.5% CMC-Na 37 mg/mL suspension

细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源

4C8	1 µM	Function Assay	0-16 h	inhibits constitutive STAT-3 and JAK2 activation	22027691
4C8	1/10 µM	Growth Inhibition Assay	24/48/72 h	inhibits cell proliferation at a concentration of 10 µM	22027691
686LN		Growth Inhibition Assay	72 h	EC50=2.05 ± 1.33 μM	25810010
8226	0.5-2 μM	Apoptosis Assay	48/72 h	induces apoptosis dose dependently	21164517
A1847	0.05-10 μM	Function Assay	24 h	reduces phosphorylated STAT3 levels	25646015
A1847	0.05-10 μM	Cell Viability Assay	72 h	reduces cell viability at the concerntration of 5 μM	25646015
AKRSL		Cell Viability Assay	72 h	IC50＞10 μM	25504635
ARPE19		Growth Inhibition Assay		IC50=24.38 μM	23531921
AS		Growth Inhibition Assay		IC50=1.53 μM	23531921
BE2		Growth Inhibition Assay		IC50=0.71 μM	23531921
Cal33		Growth Inhibition Assay	72 h	EC50=3.37 ± 0.75 μM	25810010
Cal33	0.0005-3.8 μM	Function Assay	24 h	abrogates IL-6–induced up-regulation of pSTAT3Tyr705 in a dose-dependent manner	25810010
CWR22Pc		Apoptosis Assay		IC50=0.438 μM	23942095
CWR22Rv1	800 nM	Function Assay	72 h	suppresses IL-6-induced migratory	24577942
CWR22Rv1		Apoptosis Assay		IC50=0.482 μM	23942095
DMS114		Growth Inhibition Assay		IC50=0.73 μM	24158701
DU145	0-200 nM	Function Assay	1 h	suppresses IL-6-activated Stat3 and ERK1/2 signaling	24577942
DU145	800 nM	Function Assay	72 h	suppresses IL-6-induced migratory	24577942
DU145		Apoptosis Assay		IC50=3.517 μM	23942095
GLC4		Growth Inhibition Assay		IC50=1.79 μM	24158701
GLC4	0.3/1/3 μM	Function Assay	24 h	induces G2/M cell cycle arrest	24158701
GLC4	0.3/1/3 μM	Apoptosis Assay	48 h	increases the level of cleaved-Caspase 3	24158701
H1173		Growth Inhibition Assay		IC50=2.39 μM	24158701
H526		Growth Inhibition Assay		IC50=3.08 μM	24158701
H82		Growth Inhibition Assay		IC50=1.37 μM	24158701
HD-LM2		Growth Inhibition Assay	72 h	IC50=7.844 μM	22829094
HD-LM2	0.1/0.5/1/5 μM	Function Assay	72 h	inhibits STAT3, STAT5 and STAT6 phosphorylation	22829094
HD-LM2	1/5 μM	Apoptosis Assay	72 h	induces apoptosis	22829094
HEK293		Growth Inhibition Assay		IC50=8.67 μM	23531921
HH5	0.0005-3.8 μM	Function Assay	24 h	abrogates IL-6–induced up-regulation of pSTAT3Tyr705 in a dose-dependent manner	25810010
HN5		Growth Inhibition Assay	72 h	EC50=3.81 ± 1.99 μM	25810010
IMR32		Growth Inhibition Assay		IC50=0.66 μM	23531921
KCNR		Growth Inhibition Assay		IC50=0.46 μM	23531921
KCNR	0.5/1.0/2.5 μM	Apoptosis Assay	24 h	induces an increase in caspase 3/7 activity	23531921
KCNR	0.5/1.0/2.5/5 μM	Function Assay	24 h	inhibits both endogenous constitutive and IL-6-induced STAT3 activation	23531921
KM-H2		Growth Inhibition Assay	72 h	IC50=1.308 μM	22829094
KM-H2	0.1/0.5/1/5 μM	Function Assay	72 h	inhibits STAT3, STAT5 and STAT6 phosphorylation	22829094
KM-H2	1/5 μM	Apoptosis Assay	72 h	induces apoptosis	22829094
Kms.11	0.5-2 μM	Apoptosis Assay	48/72 h	induces apoptosis dose dependently	21164517
L-428		Growth Inhibition Assay	72 h	IC50=7.947 μM	22829094
L-428	0.1/0.5/1/5 μM	Function Assay	72 h	inhibits STAT3, STAT5 and STAT6 phosphorylation	22829094
L-428	1/5 μM	Apoptosis Assay	72 h	induces apoptosis	22829094
L-540		Growth Inhibition Assay	72 h	IC50=8.216 μM	22829094
L-540	0.1/0.5/1/5 μM	Function Assay	72 h	inhibits STAT3, STAT5 and STAT6 phosphorylation	22829094
L-540	1/5 μM	Apoptosis Assay	72 h	induces apoptosis	22829094
LAN5		Growth Inhibition Assay		IC50=1.04 μM	23531921
LoVo	5 μM	Function Assay	48 h	blocks JAK2/STAT3 signaling	25954974
MO4	0.5/1/5 μM	Function Assay	6 h	inhibits P-STAT3 expression	25149535
MOVCAR-5009	0.05-10 μM	Function Assay	24 h	reduces phosphorylated STAT3 levels	25646015
MOVCAR-5447	0.05-10 μM	Function Assay	24 h	reduces phosphorylated STAT3 levels	25646015
MZ-CRC1	1 µM	Growth Inhibition Assay	0-5 d	inhibits cell growth after 1 d treatment	23056499
MZ-CRC1	1 µM	Function Assay	72 h	induces G1 blockage	23056499
MZ-CRC1	1 µM	Apoptosis Assay	48 h	induces apoptosis	23056499
N592		Growth Inhibition Assay		IC50=0.84 μM	24158701
NCI-H82	0.3/1/3 μM	Function Assay	24 h	induces G2/M cell cycle arrest	24158701
NCI-H82	0.3/1/3 μM	Apoptosis Assay	48 h	increases the level of cleaved-Caspase 3	24158701
NCI-N592	0.3/1/3 μM	Function Assay	24 h	induces G2/M cell cycle arrest	24158701
NCI-N592	0.3/1/3 μM	Apoptosis Assay	48 h	increases the level of cleaved-Caspase 3	24158701
NGP		Growth Inhibition Assay		IC50=0.56 μM	23531921
OSC19		Growth Inhibition Assay	72 h	EC50=1.26 ± 0.20 μM	25810010
OVCAR-5	0.05-10 μM	Function Assay	24 h	reduces phosphorylated STAT3 levels	25646015
OVCAR-5	0.05-10 μM	Cell Viability Assay	72 h	reduces cell viability at the concerntration of 5 μM	25646015
OVCAR-5	0.5/1/5 μM	Apoptosis Assay	48 h	induces significant apoptosis at high concerntration	25646015
OVCAR-8	0.05-10 μM	Function Assay	24 h	reduces phosphorylated STAT3 levels	25646015
OVCAR-8	0.05-10 μM	Cell Viability Assay	72 h	reduces cell viability at the concerntration of 5 μM	25646015
OVCAR-8	0.5/1/5 μM	Apoptosis Assay	48 h	induces significant apoptosis at high concerntration	25646015
PALJDL		Cell Viability Assay	72 h	IC50=2.4 μM	25504635
PC-3		Apoptosis Assay		IC50=1.755 μM	23942095
PCI-15B		Growth Inhibition Assay	72 h	EC50=0.99 ± 1.74 μM	25810010
PCI-52		Growth Inhibition Assay	72 h	EC50=1.00 ± 0.09 μM	25810010
RC165N		Apoptosis Assay		IC50=2.083 μM	23942095
RD		Growth Inhibition Assay		IC50=4.32 μM	23531921
RH17		Growth Inhibition Assay		IC50=2.51 μM	23531921
RH18		Growth Inhibition Assay		IC50=1.42 μM	23531921
Rh18	0.5/1.0/2.5 μM	Apoptosis Assay	24 h	induces an increase in caspase 3/7 activity	23531921
Rh18	0.5/1.0/2.5/5 μM	Function Assay	24 h	inhibits both endogenous constitutive and IL-6-induced STAT3 activation	23531921
RH28		Growth Inhibition Assay		IC50=4.28 μM	23531921
RH30		Growth Inhibition Assay		IC50=1.25 μM	23531921
RH36		Growth Inhibition Assay		IC50=5.37 μM	23531921
RH41		Growth Inhibition Assay		IC50=0.48 μM	23531921
SW620	5 μM	Function Assay	48 h	blocks JAK2/STAT3 signaling	25954974
SY5Y		Growth Inhibition Assay		IC50=0.36 μM	23531921
SY5Y	0.5/1.0/2.5 μM	Apoptosis Assay	24 h	induces an increase in caspase 3/7 activity	23531921
SY5Y	0.5/1.0/2.5/5 μM	Function Assay	24 h	inhibits both endogenous constitutive and IL-6-induced STAT3 activation	23531921
TC32		Growth Inhibition Assay		IC50=3.85 μM	23531921
TC32	0.5/1.0/2.5 μM	Apoptosis Assay	24 h	induces an increase in caspase 3/7 activity	23531921
TC32	0.5/1.0/2.5/5 μM	Function Assay	24 h	inhibits both endogenous constitutive and IL-6-induced STAT3 activation	23531921
TC71		Growth Inhibition Assay		IC50=4.33 μM	23531921
TPC-1	1 µM	Growth Inhibition Assay	0-4 d	inhibits cell growth after 2 d treatment	23056499
TPC-1	1 µM	Function Assay	72 h	induces G1 blockage	23056499
TT	1 µM	Growth Inhibition Assay	0-4 d	inhibits cell growth after 1 d treatment	23056499
TT	1 µM	Function Assay	72 h	induces G1 blockage	23056499
TT	1 µM	Apoptosis Assay	48 h	induces apoptosis	23056499
U251-MG	1 µM	Function Assay	0-16 h	inhibits constitutive STAT-3 and JAK2 activation	22027691
U251-MG	1/10 µM	Growth Inhibition Assay	24/48/72 h	inhibits cell proliferation at a concentration of 10 µM	22027691
U266	0.5-2 μM	Apoptosis Assay	48/72 h	induces apoptosis dose dependently	21164517
U87-MG	1 µM	Function Assay	0-16 h	inhibits constitutive STAT-3 and JAK2 activation	22027691
U87-MG	1/10 µM	Growth Inhibition Assay	24/48/72 h	inhibits cell proliferation at a concentration of 10 µM	22027691
UM SCC-1		Growth Inhibition Assay	72 h	EC50=1.67 ± 0.42 μM	25810010
UM-22A		Growth Inhibition Assay	72 h	EC50=1.32 ± 0.39 μM	25810010
UM-22A	0.0005-1.6 μM	Function Assay	24 h	abrogates IL-6–induced up-regulation of pSTAT3Tyr705 in a dose-dependent manner	25810010
UM-22B		Growth Inhibition Assay	72 h	EC50=2.66 ± 0.24 μM	25810010
UMSCC-1	0.0005-1.6 μM	Function Assay	24 h	abrogates IL-6–induced up-regulation of pSTAT3Tyr705 in a dose-dependent manner	25810010

AZD-1480 99%+

AZD-1480 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

AZD-1480 质控信息

AZD-1480 生物活性

AZD-1480 细胞研究

AZD-1480 临床研究

AZD-1480 参考文献

AZD-1480 实验方案

AZD-1480 技术信息

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AZD-1480 99%+

AZD-1480 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

AZD-1480 质控信息

AZD-1480 生物活性

AZD-1480 细胞研究

AZD-1480 临床研究

AZD-1480 参考文献

AZD-1480 实验方案

AZD-1480 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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