KB-0742 dihydrochloride

Research use only, not for human use.

KB-0742 dihydrochloride is a potent, selective and orally inhibitor of ?CDK9.

KB-0742 dihydrochloride is a potent, selective and orally inhibitor of ?CDK9.

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.Western Blot Analysis Cell 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.

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. 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).

KB-0742 dihydrochloride

Angiogenesis

CDK

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2416874-75-2

360.33

C16H27Cl2N5

>98% (HPLC)

In Vitro:?H2O : 100 mg/mL (277.52 mM)

Cl.Cl.CCC(CC)c1cc(N[C@H]2CC[C@H](N)C2)n2nccc2n1

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(-20℃)

With Ice Pack

≥ 2 years