Atuveciclib, also known as BAY1143572, is a highly selective, potent and orally available inhibitor of PTEFb/CDK9 currently in Phase I. BAY1143572 inhibits MYC and shows convincing anti-tumor activity in multiple xenograft models by the induction of apoptosis. BAY 1143572 had potent and highly selective PTEFb-kinase inhibitory activity in the low nanomolar range against PTEFb/CDK9 and an at least 50-fold selectivity against other CDKs in enzymatic assays. BAY 1143572 also showed single agent in vivo efficacy at tolerated doses in various xenograft tumor models in mice and rats upon once daily oral administration.
MedKoo Cat#: 575108
Name: Atuveciclib
CAS#: 1414943-94-4
Chemical Formula: C18H18FN5O2S
Exact Mass: 387.1165
Molecular Weight: 387.43
Elemental Analysis: C, 55.80; H, 4.68; F, 4.90; N, 18.08; O, 8.26; S, 8.27
The following data is based on the product molecular weight 387.43 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
