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KB-0742 dihydrochloride

CAS No. : 2416874-75-2

MCE 站：KB-0742 dihydrochloride

产品活性：KB-0742 dihydrochloride 是一种有效的，选择性的和具有口服活性的 CDK9 抑制剂，对 CDK9/cyclin T1 的 IC₅₀ 为 6 nM。KB-0742 dihydrochloride 对 CDK9/cyclin T1 具有选择性，其选择性是其他 CDK 激酶的 50 倍以上。KB-0742 dihydrochloride 具有有效的抗肿瘤活性。

研究领域：Cell Cycle/DNA Damage

作用靶点：CDK

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 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.

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.

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