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
- 公司名称:上海楼岚生物科技有限公司
- 联系电话:021-52996696,15000506266 15000506266
- 电子邮件:
- 国家:中国
- 产品数:4512
- 优势度:55
- 公司名称:上海泽涵生物医药科技有限公司
- 联系电话:021-61350663 13052117465
- 电子邮件:sales@zehanbiopharma.com
- 国家:中国
- 产品数:1009
- 优势度:55
- 公司名称:BOC Sciences
- 联系电话: 16314854226
- 电子邮件:info@bocsci.com
- 国家:美国
- 产品数:9923
- 优势度:65
- 公司名称:上海瀚香生物科技有限公司
- 联系电话:177-54423994 17754423994
- 电子邮件:2853530910@QQ.com
- 国家:中国
- 产品数:8011
- 优势度:62
- 公司名称:上海芮晖化工科技有限公司
- 联系电话:21-31433387 15618786686
- 电子邮件:sales@rechemscience.com
- 国家:中国
- 产品数:2990
- 优势度:58
- 公司名称:上海超岚化工科技中心
- 联系电话:021-QQ:65489617 15618227136
- 电子邮件:Sales@ATKchemical.com
- 国家:中国
- 产品数:7268
- 优势度:58
- 公司名称:北京普西唐生物科技有限公司
- 联系电话:010-60605840 18892239720
- 电子邮件:psaitong@jm-bio.com
- 国家:中国
- 产品数:12306
- 优势度:58
- 公司名称:滁州市科迈尔化工科技有限公司
- 联系电话:0550-5196001 15000891977
- 电子邮件:wj520wjxby@126.com
- 国家:中国
- 产品数:1847
- 优势度:55
- 公司名称:菏泽开发区创蠡化工科技有限公司
- 联系电话:+86-530-529 6766,+86-15666160102 15666160102
- 电子邮件:info@chuangli-chem.com
- 国家:中国
- 产品数:894
- 优势度:55
- 公司名称:Musechem
- 联系电话:+1-800-259-7612
- 电子邮件:info@musechem.com
- 国家:美国
- 产品数:4660
- 优势度:60