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199986-75-9

中文名稱(chēng) CVT 313
英文名稱(chēng) 2(BIS-(HYDROXYETHYL)AMINO)-6-(4-METHOXYBENZYLAMINO)-9-ISOPROPYL-PURINE
CAS 199986-75-9
分子式 C20H28N6O3
分子量 400.47
MOL 文件 199986-75-9.mol
更新日期 2024/12/23 09:08:08
199986-75-9 結(jié)構(gòu)式 199986-75-9 結(jié)構(gòu)式

基本信息

中文別名
化合物CVT313
CVT-313游離態(tài)
CDK2抑制劑(CVT-313)
英文別名
BAT5
NG 26
D6S82E
CVT-313
CS-2441
CVT-313, >98%
CVT-313(NG-26)
CDK2 INHIBITOR III
CVT 313
NG 26
CVT313
NG26
CVT-313 (CDK2 INHIBITOR III)
所屬類(lèi)別
生物化工:激動(dòng)劑抑制劑

物理化學(xué)性質(zhì)

沸點(diǎn)652.3±65.0 °C(Predicted)
密度1.30±0.1 g/cm3(Predicted)
儲(chǔ)存條件Sealed in dry,Store in freezer, under -20°C
溶解度≥20 mg/mL in DMSO; insoluble in H2O; ≥51.1 mg/mL in EtOH with gentle warming
酸度系數(shù)(pKa)13.95±0.10(Predicted)
形態(tài)白色固體
顏色White to off-white
InChIKeyNQVIIUBWMBHLOZ-UHFFFAOYSA-N

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302
防范說(shuō)明P280-P305+P351+P338

圖譜信息

常見(jiàn)問(wèn)題列表

生物活性
CVT-313是有效的CDK2抑制劑,在體外的IC50值為0.5 μM。它對(duì)其他非相關(guān)的、依賴(lài)于ATP的絲氨酸/蘇氨酸激酶沒(méi)有作用。
靶點(diǎn)
TargetValue
CDK2
(Cell-free assay)
0.5 μM
體外研究

CVT-313 (Cdk2 Inhibitor III) has been shown to inhibit other kinases, but at much higher IC 50 values, i.e., CDK1 (IC 50 =4.2 μM), CDK4 D1 (IC 50 =215 μM), and MAPK/PKA/PKC (IC 50 >1.25 mM), compared to CDK2 (IC 50 =0.5 μM). CVT-313 has been shown to have profound effects on cell proliferation at concentrations of 5-20 μM. CVT-313 is a potent CDK2 inhibitor, which is identified from a purine analog library with an IC 50 of 0.5 μM in vitro. Inhibition is competitive with respect to ATP (K i =95 nM), and selective CVT-313 has no effect on other, nonrelated ATP-dependent serine/threonine kinases. When added to CDK1 or CDK4, a 8.5- and 430-fold higher concentration of CVT-313 is required for half-maximal inhibition of the enzyme activity. Using normal and tumor human/murine cell lines, the effects of CVT-313 on cell proliferation is measured. The IC 50 for growth inhibition ranged from 1.25 to 20 μM.

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