|1,3-二氢-3-(1H-咪唑-5-基亚甲基)-5-甲氧基-2H-吲哚-2-酮|CsnPharm

CAS No.: 666837-93-0

3-((1H-Imidazol-5-yl)methylene)-5-methoxyindolin-2-one Catalog No. CSN20451

Synonyms: Su-9516

SU9516 (mixture) is a 3-substituted indolinone compound and a competitive inhibitor of CDC2 CDK2 and CDK4 that displaying anti-proliferative and proapoptotic properties in tumor cells. It is the mixture form of SU9516.

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技术信息

生物活性

描述Progression through the cell cycle is determined by sequential and specific phosphorylation events by holoenzymes involving cyclins and their catalytic partners, the CDKs. SU9516 (mixture) is a mixture form of SU9516. SU9516, a novel 3-substituted indolinone compound, binds to and selectively inhibits the activity of CDK2 with IC₅₀ of 22 nM. It also inhibits CDK1 and CDK4 with IC₅₀s of 40 nM and 200 nM. Continuous exposure to SU9516 (5 μM) for 24, 48, or 72 h resulted in a 4-52% decrease (P≤ 0.05) in CDK2-specific phosphorylation of pRb (retinoblastoma protein, a known CDK substrate) in RKO cells. The addition of 5 μM SU9516 produced a 27.6% decrease in RKO G₀-G₁ populations by 48 h post-drug addition and a 39.1% decrease by 72 h. A concomitant increase in RKO G₂-M populations results in a G₂-M block with G₂-M populations increasing by 13.1% over controls at 24 h to a 34.1% at 72 h post-drug addition. After continuous exposure to 5 μM SU9516 for 24, 48, and 72 h, both RKO (10-15%) and SW480 (4-22%) cells demonstrated an increase (P ≤ 0.01) in apoptosis. With inhibition of pRb phosphorylation, proliferation in both RKO and SW480 cells decreased in a dose-dependent manner at 20 h after treatment with SU9516.
动物研究
剂量
Nude mice: 2.5 mg/kg/day - 10 mg/kg/day (p.o.)

给药途径
p.o.
参考文献

动物研究
剂量	Nude mice: 2.5 mg/kg/day - 10 mg/kg/day (p.o.)
给药途径	p.o.

[1] Heady L, Fernandez-Serra M, et al. Novel structural features of CDK inhibition revealed by an ab initio computational method combined with dynamic simulations. J Med Chem. 2006 Aug 24;49(17):5141-53.
[2] Lane ME, Yu B, et al. A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells. Cancer Res. 2001 Aug 15;61(16):6170-7.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.1452 mL
- 20.7258 mL
- 41.4516 mL
- 5 mM
- 0.8290 mL
- 4.1452 mL
- 8.2903 mL
- 10 mM
- 0.4145 mL
- 2.0726 mL
- 4.1452 mL

技术信息

CAS号	666837-93-0	储存条件	粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C13H11N3O2	运输	蓝冰
分子量	241.25	别名	Su-9516

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3-((1H-Imidazol-5-yl)methylene)-5-methoxyindolin-2-one Catalog No. CSN20451

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