(+)-BAY-1251152

(+)-BAY-1251152 is an enanthiomer of BAY-1251152 with rotation (+). (+)-BAY-1251152 is a potent and selective CDK9 inhibitor with an IC50 of 3 nM. (+)-BAY-1251152 has anti-tumour activity.

Product information

CAS Number: 1610358-56-9

Molecular Weight: 404.43

Formula: C19H18F2N4O2S

Chemical Name: (+)-[(2-{[5-fluoro-4-(4-fluoro-2-methoxyphenyl)pyridin-2-yl]amino}pyridin-4-yl)methyl](imino)methyl--sulfanone

Smiles: COC1=CC(F)=CC=C1C1=CC(NC2=CC(CS(C)(=N)=O)=CC=N2)=NC=C1F

InChiKey: YZCUMZWULWOUMD-UHFFFAOYSA-N

InChi: 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)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 113.3 mg/mL (280.15 mM; Need ultrasonic and warming).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

(+)-BAY-1251152 (Example 2) inhibits HeLa, HeLa-MaTu-ADR, NCI-H460, DU145, Caco-2, B16F10, A2780 and MOLM-13 cells proliferation with IC50 values of 110 nM, 33 nM, 75 nM, 33 nM, 62 nM, 240 nM, 110 nM and 29 nM, respectively. An efficient inhibition of the proliferation of both ABC (Activated B-cell type) and GCB (Germinal-centre B-cell type) subtypes of diffuse large B-cell lymphoma (DLBCL) by (+)-BAY-1251152 (Compound A').

In Vivo:

(+)-BAY-1251152 (Compound A’; 10 mg/kg; intravenous injection; once every seven days; for 14 days; female SCID mice) treatment reaches a Treatment to Control ratios (T/C) by area of 0.29 and a T/C by weight of 0.24. (+)-BAY-1251152 inhibits tumour growth and had good tolerability.

Products are for research use only. Not for human use.