基本属性 生物活性靶点体外研究体内研究 用途与合成方法 CS-2259 价格(试剂级) 供应商 供应信息
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CS-2259

CS-2259

中文名称:CS-2259
英文名称:CDKI-73
CAS号:1421693-22-2
分子式:C15H15FN6O2S2
分子量:394.45
EINECS号:
Mol文件:1421693-22-2.mol
CS-2259 结构式

CS-2259 性质

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(最大浓度 mg/mL);131.83(最大浓度 mM)
形态 固体
酸度系数(pKa) 10.06±0.60(Predicted)
颜色 浅黄至黄色

CS-2259 用途与合成方法

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。
TargetValue
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

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.

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.

CS-2259 价格(试剂级)

更新日期 产品编号 产品名称 CAS号 包装 价格
2024-11-08 HY-12445 1 mg 1600
2024-11-08 HY-12445 CS-2259 1421693-22-2 2mg 2333

CS-2259供应商 更多

无锡东禾医药科技有限公司
现货
联系电话:63313187 15358055255
产品介绍:
英文名称:CDKI-73
CAS:1421693-22-2
纯度:98%
包装信息:10mg/;25mg/;50mg/;100mg/
库存量:>1g
现货日期:2024/12/24 22:26:01
上海楼岚生物科技有限公司
联系电话:021-52996696,15000506266 15000506266
产品介绍:
英文名称:CDKI-73
CAS:1421693-22-2
纯度:>98%
包装信息:5MG;10MG;50MG;100MG,1G,5G
备注:2g
上海泽涵生物医药科技有限公司
联系电话:021-61350663 13052117465
产品介绍:
英文名称:CDKI-73
CAS:1421693-22-2
纯度:98%
包装信息:5g/;10g/
上海瀚香生物科技有限公司
联系电话:177-54423994 17754423994
产品介绍:
英文名称:CDKI-73
CAS:1421693-22-2
纯度:98% HPLC LCMS
包装信息:1G;100G
备注:量大优惠,现货促销
上海芮晖化工科技有限公司
大货
联系电话:21-31433387 15618786686
产品介绍:
CAS:1421693-22-2
纯度:98%
包装信息:1g;5g
备注:现货优势供应

最新发布供应信息

1421693-22-2CDKI-73
上海嘉定区澄浏公路52号 2024-12-25
化合物 CDKI-73|T14919|TargetMol
TargetMol中国(陶术生物) 2024-12-12