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Atuveciclib

Catalog No. T10464 CAS 2923012-24-0

Synonyms: BAY-1143572

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].

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Atuveciclib, CAS 2923012-24-0

Pack Size	Availability	Price/USD	Quantity
100 mg	10-14 weeks	$ 1,510.00

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Biological Description

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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].
Targets&IC50	CDK5-p35:1600 nM, CDK9-CyclinT1:13 nM, CDK9-CyclinT1:6 nM, CDK1-CyclinB:1100 nM, CDK2-CyclinE:1000 nM, CDK3-CyclinE:890 nM
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.

Synonyms	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)

References and Literature

1. Lücking U, et al. Identification of Atuveciclib (BAY 1143572), the First Highly Selective, Clinical PTEFb/CDK9 Inhibitor for the Treatment of Cancer. ChemMedChem. 2017 Nov 8;12(21):1776-1793.

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Keywords

Atuveciclib 2923012-24-0 Cell Cycle/Checkpoint CDK BAY1143572 BAY-1143572 BAY 1143572 inhibitor inhibit

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