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Pack Size | Price | Availability | Quantity |
---|---|---|---|
100 mg | $1,510 | 10-14 weeks |
Description | Atuveciclib (BAY-1143572) is a potent and highly selective, oral PTEFb / CDK9 inhibitor that inhibits CDK9 / CycT1 with an IC 50 of 13 nM [1]. |
In vitro | Positive transcription elongation factor b (PTEFb), comprising a CDK9-cyclin heterodimer with cyclin T1, cyclin K, cyclin T2a, or cyclin T2b as partners, demonstrates significant antiproliferative effects on HeLa cells (IC 50 =920 nM) and MOLM-13 cells (IC 50 =310 nM) when targeted with Atuveciclib (BAY-1143572) [1]. |
In vivo | In vivo studies using the MOLM-13 xenograft mouse model show that Atuveciclib (BAY-1143572) demonstrates significant antitumor activity. Administering Atuveciclib daily at doses of 6.25 or 12.5 mg/kg leads to dose-dependent tumor suppression, with treatment-to-control (T/C) ratios of 0.64 and 0.49, respectively (p<0.001). Higher doses of 20 or 25 mg/kg result in even stronger antitumor effects, with T/C ratios dropping to 0.41 and 0.31, respectively (p<0.001), and the 25 mg/kg dose being the highest tolerated by the nude mice. Additionally, dosing Atuveciclib at 25 or 35 mg/kg on a schedule of three days on and two days off yields T/C ratios of 0.33 and 0.20, respectively (p<0.001). The compound's tolerability is confirmed by a less than 10% average reduction in body weight throughout the study period. Pharmacokinetic evaluation in rats reveals Atuveciclib has a low blood clearance rate of 1.1 L/kg per hour. |
Alias | BAY-1143572 |
Molecular Weight | 387.43 |
Formula | C18H18FN5O2S |
Cas No. | 2923012-24-0 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 128.5 mg/mL (331.67 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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