BAY 1251152

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BAY 1251152 是第一个有效的、选择性的、口服的 PTEFb/CDK9 抑制剂，生化 IC50 为 9 nM，MOLM13 细胞 IC50 为 29 nM。

BAY 1251152 is the first potent, selective, orally available PTEFb/CDK9 inhibitor with biochemical IC50 of 9 nM and MOLM13 cell IC50 of 29 nM, displays> 50-fold selectivity against other CDKs;exhibits broad anti-proliferative activity against a panel of tumour cell lines with sub-micromolar IC50 values; demonstrates excellent efficacy in xenograft models (e.g. MOLM13) in mice and rats.Blood Cancer Phase 1 Clinical.

——

Animal Model:Female SCID mice with OCI-LY-3 cells Dosage:10 mg/kg Administration:Intravenous injection; once every seven days; for 14 days Result:Inhibited tumour growth and had good tolerability.

+)-BAY 1251152

Cell Cycle/DNA Damage

CDK

CDK

Cancer

Blood cancer

1610358-56-9

404.436

C19H18F2N4O2S

>98% (HPLC)

DMSO : 113.3 mg/mL. 280.15 mM

N=S(CC1=CC(NC2=NC=C(F)C(C3=CC=C(F)C=C3OC)=C2)=NC=C1)(C)=O

(+)-5-Fluoro-4-(4-fluoro-2-methoxyphenyl)-N-[4-[(S-methylsulfonimidoyl)methyl]pyridin-2-yl]pyridin-2-amine

(-20℃)

With Ice Pack

≥ 2 years