BAY-1251152 (BAY 1251152)

BAY-1251152 (BAY 1251152)

$100.00$450.00

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Description

Background Information:

BAY 1251152 (BAY-1251152) is the next-generation, potent and highly selective CDK9/P-TEFb inhibitor in clinical evaluation. In comparison to BAY 1143572 (the first oral CDK9/P-TEFb inhibitor), BAY 1251152 shows significantly increased biochemical (IC50 CDK9 = 3 nM) and cellular potency (IC50 MOLM13 = 29 nM), and an increased selectivity against CDK2 as well as high permeability and no efflux. The significantly reduced therapeutic dosage and high solubility of BAY 1251152 enable the desired i.v. application. It demonstrated excellent in vivo efficacy upon i.v. treatment in xenograft models (e.g. MOLM13) in mice and rats (ref 1). Cyclin-dependent kinase 9 (CDK9), a subunit of the positive transcription elongation factor b (P-TEFb) complex, regulates gene transcription elongation by phosphorylating the carboxy-terminal domain (CTD) of RNA polymerase II (RNAPII). The deregulation of CDK9/P-TEFb has implicated in many cancer types.

Reference:

1. Ulrich T. Luecking, et al, Identification of potent and highly selective PTEFb inhibitor BAY 1251152 for the treatment of cancer: from p.o. to i.v. application via scaffold hops, In: Proceedings of the American Association for Cancer Research Annual Meeting 2017; 2017 Apr 1-5; Washington, DC. Philadelphia (PA): AACR; Cancer Res 2017;77(13 Suppl):Abstract nr 984. doi:10.1158/1538-7445.AM2017-984.

APIM050108: BAY-1251152 (BAY 1251152)

CAS No.: 1610358-56-9.
Molecular Formula: C19H18F2N4O2S.
Molecular Weight: 404.4.
Purity: >99% by HPLC (at 214 and 254 nm).
QC: HPLC-MS, H-NMR, and Quantitative Elemental Analysis Report.
Solubility: Refer to Certificate of Analysis.
Storage: Refer to Certificate of Analysis.

Additional information

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USA

Size

10 mg, 5 mg, 50 mg

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