bay-1251152-1610358-53-6

InvivoChem Cat #:V4202CAS #:1610358-53-6 Purity >=98%

Description: (+/-)-BAY-1251152 is a racemic mixture of BAY-1251152 which is a novel, potent and highly selective PTEF/CDK9 inhibitor. BAY-1251152 shows significantly increased biochemical (IC50 CDK9 = 3 nM) and cellular potency (IC50 MOLM13 = 29 nM), increased selectivity against CDK2 as well as high permeability and no efflux. The significantly reduced therapeutic dose and high solubility of BAY 1251152 enable the desired i.v. application. BAY 1251152 demonstrated excellent efficacy upon i.v. treatment in xenograft models (e.g. MOLM13) in mice and rats. BAY 1251152 is currently being evaluated in Phase I studies (NCT02635672; NCT02745743) to determine the safety, tolerability, pharmacokinetics and initial pharmacodynamic biomarker response in patients with advanced cancer. PTEFb/CDK9 mediated transcription of short-lived anti-apoptotic survival proteins like Mcl-1 and Myc plays a critical role in cancer cell growth and survival in various tumor entities including AML. In addition, these survival proteins play important roles in the development of resistance to chemotherapy.

Description:

References: AACR; Cancer Res 2017; 77(13 Suppl):Abstract nr 984. doi:10.1158/1538-7445.AM2017-984

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Related CAS#:1610358-56-9 (+)-BAY-1251152; 1610358-59-2 (-)-BAY-1251152

-20C for 3 years in powder form

Synonym: (+/-)-BAY-1251152; (+/-)-BAY 1251152; (+/-)-BAY1251152; (-)-BAY-1251152; BAY-1251152; BAY 1251152; BAY1251152; (+)-BAY-1251152.
IUPAC/Chemical Name: (+/-)-5-Fluoro-4-(4-fluoro-2-methoxyphenyl)-N-[4-[(S-methylsulfonimidoyl)methyl]pyridin-2-yl]pyridin-2-amine
InChi Key: YZCUMZWULWOUMD-UHFFFAOYSA-N
InChi Code: InChI=1S/C19H18F2N4O2S/c1-27-17-8-13(20)3-4-14(17)15-9-19(24-10-16(15)21)25-18-7-12(5-6-23-18)11-28(2, 22)26/h3-10, 22H, 11H2, 1-2H3, (H, 23, 24, 25)
SMILES Code: N=S(CC1=CC(NC2=NC=C(F)C(C3=CC=C(F)C=C3OC)=C2)=NC=C1)(C)=O