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SU9516,≥95% (HPLC)

别名:3- [1-(3H-咪唑-4-基)-甲基-(Z)-亚烷基] -5-甲氧基-1,3-二氢-吲哚-2-酮;3-[1-(3H-Imidazol-4-yl)-meth-(Z)-ylidene]-5-methoxy-1,3-dihydro-indol-2-one

CAS号 666837-93-0;经验分子式(希尔表示法) C13H11N3O2;分子量 241.25
货号(SKU): 572650
CAS号: 666837-93-0
MDL号: MFCD17010284
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¥1,767.34

产品描述

一种强力的有选择性的周期蛋白依赖性激酶(CDKs)抑制剂。

General description

A cell-permeable 3-substituted indolinone compound that displays anti-proliferative and proapoptotic properties in tumor cells. Acts as a potent, selective, reversible, and ATP-competitive inhibitor of cyclin dependent kinases (Cdks; IC50 = 22 nM for Cdk2/A; 40 nM for Cdk1/B; 200 nM for Cdk4/D1). It shows no significant effect (IC50 >10 µM) on the activities of PKC, p38, PDGFRβ, or EGFR. Inhibits the proliferation of growth factor-stimulated colon carcinoma cells by binding to Cdk2 and preventing the phosphorylation of pRb and its dissociation from E2F.

A cell-permeable, 3-substituted indolinone compound that displays anti-proliferative and pro-apoptotic properties in tumor cells. Acts as a potent, selective, reversible, and ATP-competitive inhibitor of cyclin dependent kinases (Cdks) (IC50 = 22 nM for Cdk2/A; 40 nM for Cdk1/B; 200 nM for Cdk4/D1). Exhibits no significant effect on the activities of PKC, p38, PDGFRβ, or EGFR (IC50 >10 µM). Reported to inhibit the proliferation of growth factor-stimulated colon carcinoma cells by binding to Cdk2 and preventing the phosphorylation of pRb and its dissociation from E2F.

包装

5 mg in Plastic ampoule

Biochem/physiol Actions

Cell permeable: yes

Primary Target
Cdk2/A

Product competes with ATP.

Reversible: yes

Target IC50: 22 nM for Cdk2/A; 40 nM for Cdk1/B; 200 nM for Cdk4/D1

Warning

Toxicity: Carcinogenic / Teratogenic (D)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Yu, B., et al. 2002. Biochem. Pharmacol.64, 1091.
Lane, M.E., et al. 2001. Cancer Res.61, 6170.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

性质

Quality Level  100
assay  ≥95% (HPLC)
form  solid
mfr. no.  Calbiochem®
storage condition  OK to freeze
 protect from light
storage conditions  +2C to +8C
color  yellow to orange
solubility  DMSO: 10 mg/mL
shipped in  ambient


安全信息

WGK德国 WGK 1
商品规格
属性名称属性值
储存温度 Storage temp.2-8°C冷藏
全球实时库存 Availability √美国St. Louis ≥ 33 | 欧洲Eur. ≥ 27 | 東京Tokyo ≥ 9 | 香港与北京 ≥ 16