Atuveciclib

SKU: orb1309946

Description

Atuveciclib Racemate

Research Area

Cell Biology

Key Properties

• CAS Number: 1414943-88-6
• MW: 387.43
• Purity: 98.80%
• Formula: C₁₈H₁₈FN₅O₂S
• SMILES: COc1cc(F)ccc1-c1ncnc(Nc2cccc(CS(C)(=N)=O)c2)n1
• Target: CDK
• Solubility: DMSO:100 mg/mL (258.11 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (10.32 mM)

Bioactivity

• Target IC50:
  Antiproliferative:310 nM(MOLM-13 cells)|Antiproliferative:920 nM(HeLa cells)|P-TEFb/CDK9:13 nM|Apoptosis:385 nM(AML cell lines)
• In Vivo:
  Atuveciclib (BAY-1143572) significantly enhances its effectiveness when used with various chemotherapeutics across different solid tumor models. Additionally, it reduces MYC mRNA levels in the blood cells of treated rats, suggesting the potential of using MYC as a pharmacodynamic marker during clinical trials. When administered orally once daily, Atuveciclib demonstrates efficacy as a single agent, achieving partial or complete remission in most AML (acute myeloid leukemia) xenograft models in both mice and rats, proving its potency and tolerability at certain doses.
• In Vitro:
  Atuveciclib (BAY-1143572) exhibits a potent and highly selective inhibitory effect on PTEFb-kinase, specifically against PTEFb/CDK9, in the low nanomolar range, demonstrating at least 50-fold higher selectivity over other CDKs. The compound effectively inhibits the proliferation of seven AML cell lines, both with and without MLL rearrangements, evidenced by a median IC50 of 385 nM (ranging between 230-1100 nM), and it also triggers apoptosis. Furthermore, Atuveciclib (BAY-1143572) differentiates itself by showing significant selectivity against a broad array of non-CDK kinases, coupled with wide-ranging antiproliferative effects across various tumor cell lines indicated by sub-micromolar IC50 values. Notably, it leads to the concentration-dependent inhibition of RNA polymerase II phosphorylation, subsequently diminishing MYC mRNA and protein levels.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CDK9, CDK9/CycT1, CDK3/cyclinE, CDK1/CyclinB, CDK, CDK5/p35, CDK2/CyclinE, Cyclin dependent kinase, BAY1143572, BAY-1143572, BAY-1143572 Racemate, BAY 1143572, Atuveciclib, Atuveciclib Racemate, Inhibitor, inhibit

Compound Identifiers

PubChem CID

71618220