SU9516

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Chemical Structure| 377090-84-1 同义名 : -
CAS号 : 377090-84-1
货号 : A269439
分子式 : C13H11N3O2
纯度 : 99%+
分子量 : 241.245
MDL号 : MFCD17010284
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(435.24 mM)，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：
生物活性
靶点

  • CDK4

    CDK4, IC50:200 nM

  • CDK2

    CDK2, IC50:22 nM

  • CDK1

    CDK1, IC50:40 nM
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, 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[3].
作用机制 SU9516’s planar structure binds to the catalytic domain of CDK2. The imidazole ring of SU9516 occupies the sugar-binding region. The N3 nitrogen on SU9516 may interact favorably with the side chain amino acid Lys89.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.15mL

0.83mL

0.41mL

20.73mL

4.15mL

2.07mL

41.45mL

8.29mL

4.15mL
参考文献

[1]Gao N, Kramer L, et al. The three-substituted indolinone cyclin-dependent kinase 2 inhibitor 3-[1-(3H-imidazol-4-yl)-meth-(Z)-ylidene] -5-methoxy-1,3-dihydro-indol-2-one (SU9516) kills human leukemia cells via down-regulation of Mcl-1 through a transcriptional mechanism. Mol Pharmacol. 2006 Aug;70(2):645-55.

[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.

[3]Lane ME, Yu B, Rice A, Lipson KE, Liang C, Sun L, Tang C, McMahon G, Pestell RG, Wadler S. A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells. Cancer Res. 2001 Aug 15;61(16):6170-7. PMID: 11507069.