CS-2259
- CAS号:1421693-22-2
- 英文名:CDKI-73
- 中文名:CS-2259
- CBNumber:CB53034461
- 分子式:C15H15FN6O2S2
- 分子量:394.45
- MOL File:1421693-22-2.mol
- 沸点 :642.9±65.0 °C(Predicted)
- 密度 :1.524±0.06 g/cm3(Predicted)
- 储存条件 :Store at -20°C
- 溶解度 :DMSO:52.0(Max Conc. mg/mL);131.83(Max Conc. mM)
- 形态 :Solid
- 酸度系数(pKa) :10.06±0.60(Predicted)
- 颜色 :Light yellow to yellow
CS-2259性质、用途与生产工艺
- 生物活性 CDKI-73 (LS-007) 是一种有效的 CDK 抑制剂，对CDK1、CDK2、CDK4和CDK9的IC50值分别为8.17 nM，3.27 nM，8.18 nM和5.78 nM。CDKI-73 可诱导癌细胞的凋亡。CDKI-73 是一种口服生物利用型且高效的 CDK9 抑制剂，可用于治疗急性髓细胞性白血病。
-
靶点
Target Value CDK2
(Cell-free assay)3.27 nM CDK9
(Cell-free assay)5.78 nM CDK1
(Cell-free assay)8.17 nM CDK4
(Cell-free assay)8.18 nM -
体外研究
CDKI-73 is highly cytotoxic to primary leukemia cells derived from CLL patients (mean LD 50 = 0.08 μM) and shows>500-fold selectivity for primary leukemia cells over normal B-lymphocytes (LD 50 = 40.5 μM).
CDKI-73 (0.1 μM, 4 h) inhibits the phosphorylation of serine 2 of RNA polymerase II and MCL1 protein expression in CLL cells.
CDKI-73 induced caspase-dependent apoptosis that was preceded by dephosphorylation of cdk9 and serine 2 of RNA polymerase II.
CDKI-73 is highly effective against all cell lines tested with an IC 50 in the range of 0.012-0.517 μM; in particular three MLL-AML cell lines, namely MOLM13, MV4-11 and THP-1, were highly sensitive to CDKI-73 with IC 50 values <0.062 μM.
Cell Viability Assay.
Cell Line: CLL cells. Concentration: 0-1 μM. Incubation Time: 48 h. Result: Shows preferential cytotoxicity in CLL cells. -
体内研究
CDKI-73 (25, 50, 100 mg/kg) markedly decreases tumor growth in a dose-dependent manner and results in a prolongation of animal life span (P < 0.001) without causing body weight loss and other overt toxicities..
Animal Model: MV4-11 tumor bearing mice. Dosage: 25 mg/kg. Administration: Orally once everyday for 33 days. Result: Caused a remarkable delay in tumor growth compared to vehicle-treated mice, as reflected in a percentage for the mean tumor volume in treated to control mice of 43% at day 31. Animal Model: Balb/C mice aged 6-8 weeks. Dosage: 2 mg/kg (IV), 10, 20 and 40 mg/kg (PO). (Pharmacokinetic Analysis.) Administration: IV and PO, single dose. Result: The C max increased from 1.29 to 3.66 μM at a mean time of 1 h and the area under the curve (AUC) of CDKI-73 increased from 3.51 to 12.8 μM.h when the oral dose was escalated from 10 to 40 mg/kg.
CDKI-73 was eliminated from plasma with a mean terminal half-life (T1/2) of 2 h. Its oral bioavailability (F) ranged from 54 to 85% across the three doses.
- 更新日期：2024/11/08
- 产品编号：HY-12445
- 产品名称：Asnuciclib
- CAS编号：
- 包装：1 mg
- 价格：1600元
- 更新日期：2024/11/08
- 产品编号：HY-12445
- 产品名称：CS-2259 CDKI-73
- CAS编号：1421693-22-2
- 包装：2mg
- 价格：2333元
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- 公司名称：MedChemExpress
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