货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
V57881-1ml	10mM in DMSO	￥4010.00 V57881-1ml ￥4010.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

V57881-1ml

10mM in DMSO

￥4010.00

货期：3-5天

产品描述：

KB-0742 is a potent, selective and orally active CDK9 inhibitor with an IC50 of 6 nM for CDK9/cyclin T1. KB-0742 is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 has potent anti-tumor activity.

靶点：

CDK9/cyclinT1:6 nM (IC50); cdk2/cyclin A:397 nM (IC50); Cdk5/p25:1820 nM (IC50); CDK7/cyclin H:1510 nM (IC50); CDK3/Cyclin E:1420 nM (IC50); CDK1/cyclin A:2980 nM (IC50)

体外研究：

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.

体内研究：

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 GR50s 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.

参考文献：

1. André Richters, et al. Modulating Androgen Receptor-Driven Transcription in Prostate Cancer with Selective CDK9 Inhibitors. Cell Chem Biol. 2020 Oct 20;S2451-9456(20)30380-9.
2. Freeman DB, et al. Discovery of KB-0742, a Potent, Selective, Orally Bioavailable Small Molecule Inhibitor of CDK9 for MYC-Dependent Cancers. J Med Chem. 2023 Dec 14;66(23):15629-15647.

保存条件：

-80°C 6个月;-20°C 1个月

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	3.479 ml	17.397 ml	34.795 ml
5 mM	0.696 ml	3.479 ml	6.959 ml
10 mM	0.348 ml	1.74 ml	3.479 ml
50 mM	0.07 ml	0.348 ml	0.696 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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