计算溶液所需的质量、体积或浓度。
为什么选择此级别
提供 ≥99% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
2-8°C储存,干燥。低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
KB-0742 dihydrochloride is a potent, selective and orally active CDK9 inhibitor with an IC 50 of 6 nM for CDK9/cyclin T1 . KB-0742 dihydrochloride is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 dihydrochloride has potent anti-tumor activity
In Vitro
KB-0742 (6 hours; 0.1-10 μM; 22Rv1 cells) treatment significant reduction of downstream phosphorylation of RNA Pol II at Ser2 and Ser7, and diminished phosphorylation at Ser5. Global androgen receptor (AR)-FL and AR-V protein levels are significantly reduced starting at 6 h treatment time, which is accompanied by the reduction of phospho-AR levels (Ser81). KB-0742 (48-72 hours) treatment shows cytostatic effects in prostate cancer and leukemia cell lines. KB-0742 shows antiproliferative activity with GR 50 s of 0.183 μM and 0.288 μM for 22Rv1 cells and MV-4-11 AML cells, respectively. In 22Rv1 cells, KB-0742 rapidly downregulates nascent transcription, preferentially depleting short half-life transcripts and AR-driven oncogenic programs. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: 22Rv1 cells Concentration: 0.1 μM, 0.5 μM, 1 μM, 10 μM Incubation Time: 6 hours Result: Significant reduction of downstream phosphorylation of RNA Pol II at Ser2 and Ser7, and diminished phosphorylation at Ser5.
In Vivo
KB-0742 (3-30 mg/kg; p.o.; daily; over 21 days) is well tolerated even at high dose, while significantly reducing tumor burden in 22Rv1 human prostate cancer cell line-derived xenograft (CDX) models . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male CB17-SCID mice injected with 22Rv1 human prostate cancer cells Dosage: 3 mg/kg, 10 mg/kg, and 30 mg/kg Administration: p.o.; daily; over 21 days Result: Significantly reduced tumor growth in castration-resistant prostate cancer (CRPC).
Form:Solid
IC50& Target:CDK9/cyclinT1 6 nM (IC 50 )
规格
别名
KB-0742 二盐酸盐
规格或纯度
≥99%
英文名称
KB-0742 dihydrochloride
生化机理
KB-0742 二盐酸盐是一种强效、选择性和口服活性 CDK9 抑制剂，对 CDK9/cyclin T1 的 IC 50 为 6 nM。KB-0742 二盐酸盐对 CDK9/cyclin T1 具有选择性，选择性大于其他 CDK 激酶的 50 倍。KB-0742 二盐酸盐具有
储存条件
2-8°C储存,干燥
运输条件
低温运输
作用类型
抑制剂
纯度
≥99%
名称和识别符
分子类型
小分子
IUPAC Name
(1S,3S)-3-N-(5-pentan-3-ylpyrazolo[1,5-a]pyrimidin-7-yl)cyclopentane-1,3-diamine;dihydrochloride
INCHI
1S/C16H25N5.2ClH/c1-3-11(4-2)14-10-16(19-13-6-5-12(17)9-13)21-15(20-14)7-8-18-21;;/h7-8,10-13,19H,3-6,9,17H2,1-2H3;2*1H/t12-,13-;;/m0../s1
InChi Key
OTUPXOLLHVLWQF-NJHZPMQHSA-N
Smiles
CCC(CC)C1=NC2=CC=NN2C(=C1)NC3CCC(C3)N.Cl.Cl
PubChem CID
分子量
360.33
技术文档
高级数据
三维结构
交互式化学结构模型
化学和物理性质
溶解性
H2O : 100 mg/mL (277.52 mM; Need ultrasonic) DMSO : 62.5 mg/mL (173.45 mM; Need ultrasonic)
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
常见问题
本产品的纯度是多少？
本产品的化学纯度（含量）为 ≥99%。批次的具体数值以分析证书（COA）为准。
本产品应如何储存？
请于2–8 °C、干燥条件下保存。请与干燥剂一同密封保存，本品对湿气敏感。
本产品如何运输？
本产品采用湿冰冷藏运输。收货后请立即拆包，并按上述储存条件保存。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 2416874-75-2，分子式为 C16H27Cl2N5，分子量为 360.33 g/mol。InChIKey OTUPXOLLHVLWQF-NJHZPMQHSA-N。
如何获取批次专用COA？
每个订单都会随附分析证书（COA），您也可以从账户订单历史中下载。如需订购前的COA，请联系您的客户代表，或使用PDP上的"申请COA"按钮——我们将提供代表性批次的COA。
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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