≥98% for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
🌡
Storage & shipping
Store at -20°C Ships Ice chest + Ice pads Check lot-specific COA for exact specifications.
📋
Quality documents
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
📚
Literature proof
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Descripción general
Information
Atuveciclib (BAY-1143572) is potent and highly selectivePTEFb/CDK9inhibitor withIC50values of 13 nM for CDK9/CycT and the ratio of IC50 values for CDK2/CDK9 is about 100. Outside the CDK family, It inhibits GSK3 kinase with IC50 values of 45 nM and 87 nM for GSK3α and GSK3β respectively.
BAY\u20051143572 is a potent and highly selective CDK9 inhibitor (IC50 CDK9/CycT1: 13\u2005nM, ratio of IC50 values CDK2/CDK9: 100). Outside the CDK family, submicromolar inhibitory activity was only recorded against GSK3 kinase (IC50 GSK3α: 45\u2005nM, GSK3β: 87\u2005nM). BAY\u20051143572 demonstrates antiproliferative activity against HeLa cells (IC50 = 920\u2005nM) and MOLM-13 cells (IC50 = 310\u2005nM). It also demonstrates improved Caco-2 permeability and a decreased efflux ratio (PappA→B: 35\u2005nm/s, ER: 6) relative to lead compound BAY‐958 (PappA→B: 22\u2005nm/s, ER: 15).
In vivo
In an in\u2005vivo pharmacokinetic study in rats, BAY\u20051143572 showed low blood clearance (CLb 1.1\u2005L/h/kg). The volumes of distribution (Vss) of BAY\u20051143572 is 1.0\u2005L/kg. BAY\u20051143572 shows significantly improved oral bioavailability of 54\u2009%. The blood/plasma ratios is about 1. It does not show significant inhibition of cytochrome P450 activity, with IC50 values >20\u2005μM. The administration of BAY 1143572 in immunocompromized NOD/Shi-scid/IL-2Rγ (NOG) mice xenografted with patient-derived ATL cells greatly reduced the infiltration of ATL cells into organs, such as liver and bone marrow. Decreased human soluble IL2R levels in serum were also observed, which indicated a reduction of ATL tumor burden.
Atuveciclib (BAY-1143572) is potent and highly selective PTEFb/CDK9 inhibitor with IC50 values of 13 nM for CDK9/CycT and the ratio of IC50 values for CDK2/CDK9 is about 100. Outside the CDK family, It inhibits GSK3 kinase with IC50 values of 45 nM and 87
Condiciones de almacenamiento de almacenamiento
Store at -20°C
Enviado en
Ice chest + Ice pads
Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.
This compound belongs to the class of organic compounds known as anisoles. These are organic compounds containing a methoxybenzene or a derivative thereof.
External Descriptors
Not available
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.
We use cookies to ensure the website functions properly and, where permitted, to improve your experience. You can manage your preferences at any time in Settings. Learn more in our Cookie Policy.
Shall we send you a message when we have discounts available?
Remind me later
Thank you! Please check your email inbox to confirm.
Products are supplied to verified businesses, institutions, and qualified professionals for research and development use only. Not for use in humans, animals, diagnosis, or therapy.
J2515098
