|(Z)-3-((1H-咪唑-4-基)亚甲基)-5-甲氧基吲哚啉-2-酮|CsnPharm

CAS No.: 377090-84-1

(Z)-3-((1H-Imidazol-4-yl)methylene)-5-methoxyindolin-2-one Catalog No. CSN16666

Synonyms: SU9516

SU9516 is a selective and potent CDK2 inhibtor with IC50 of 22 nM, less potent for CDK1/CDK4 (IC50=40/200 nM), and with no inhibition on PKC, EGFR, p38MAPK, etc.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 CDK4

IC50:200nM CDK2

IC50:22nM CDK1

IC50:40nM
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.
动物研究
剂量
Nude mice: 2.5 mg/kg/day - 10 mg/kg/day^[3] (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^[3] (p.o.)
给药途径	p.o.

[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.

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

377090-84-1

储存条件

粉末: 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

SU9516

溶解度

DMSO	48.0 mg/mL (199.0 mM)
Water	Insoluble
Ethanol	10.0 mg/mL (41.5 mM) warming

动物实验配方

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靶点	Description	IC50
CDK4		IC50:200nM
CDK2		IC50:22nM
CDK1		IC50:40nM

(Z)-3-((1H-Imidazol-4-yl)methylene)-5-methoxyindolin-2-one Catalog No. CSN16666

靶点选择性

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