BMS-509744 ( PD 0332991 )

产品货号. M21885 CAS No. 439575-02-7

BMS-509744 是一种有效的、选择性的 ATP 竞争性 Itk 抑制剂，IC50 为 19 nM。

纯度: >98% (HPLC)

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

规格	价格/人民币	库存	数量
2MG	￥947	有现货
25MG	￥7942	有现货
50MG	￥10323	有现货
100MG	￥15570	有现货
500MG	获取报价	有现货
1G	获取报价	有现货

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生物学信息

产品名称

BMS-509744
注意事项

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
产品简述

BMS-509744 是一种有效的、选择性的 ATP 竞争性 Itk 抑制剂，IC50 为 19 nM。
产品描述

BMS-509744 reduces T-cell receptor-induced functions including PLCγ1 tyrosine phosphorylation, calcium mobilization, IL-2 secretion, and T-cell proliferation in vitro in both human and mouse cells. BMS-488516 and BMS-509744 potently inhibit Itk in vitro with IC50 values of 96 and 19 nM, respectively. Both compounds exhibit competitive kinetics with respect to ATP, suggesting that they bind to the ATP binding site of the Itk kinase domain.
体外实验

BMS-509744 reduces T-cell receptor-induced functions including PLCγ1 tyrosine phosphorylation, calcium mobilization, IL-2 secretion, and T-cell proliferation in vitro in both human and mouse cells. BMS-488516 and BMS-509744 potently inhibit Itk in vitro with IC50 values of 96 and 19 nM, respectively. Both compounds exhibit competitive kinetics with respect to ATP, suggesting that they bind to the ATP binding site of the Itk kinase domain.
体内实验

BMS-509744 and BMS-488516 suppress the production of IL-2 induced by anti-T-cell receptor antibody administered to mice. BMS-509744 exhibits a 50% inhibitory capacity when dosed at 50 mg/kg, irrespective of the amount of induction antibody. BMS-509744 also significantly diminishes lung inflammation in a mouse model of ovalbumin-induced allergy/asthma.
同义词

PD 0332991
通路

Angiogenesis
靶点

CDK
受体

MAPK/DYRK1A
研究领域

——
适应症

——

化学信息

CAS Number

439575-02-7
分子量

447.53
分子式

C??H??N?O?
纯度

>98% (HPLC)
溶解度

DMSO : 5 mg/mL (11.17 mM; ultrasonic and adjust pH to 3 with HCl)；H2O : 0.1 mg/mL (0.22 mM; Need ultrasonic)
SMILES

O=C1C(C(C)=O)=C(C2=CN=C(N=C2N1C3CCCC3)NC4=CC=C(N5CCNCC5)C=N4)C
化学全称

——

运输与储存

储存条件

(-20℃)
运输条件

With Ice Pack
稳定性

≥ 2 years

参考文献

1. Fry DW, et al. Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Mol Cancer Ther. 2004 Nov;3(11):1427-38. 2. Katsumi Y, et al. Sensitivity of malignant rhabdoid tumor cell lines to PD 0332991 is inversely correlated with p16 expression. Biochem Biophys Res Commun, 2011, 413(1), 62-68. 3. Goel S, et al. CDK4/6 inhibition triggers anti-tumour immunity. Nature. 2017 Aug 24;548(7668):471-475.

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