1. Cell Cycle/DNA Damage
  2. CDK

BAY-1143572 Racemate 

Cat. No.: HY-12871 Purity: >98.0%
Handling Instructions

BAY 1143572 is a highly selective, potent and orally available inhibitor of PTEFb/CDK9; inhibits the proliferation of AML cell lines with a median IC50 of 385 nM.

For research use only. We do not sell to patients.

BAY-1143572 Racemate Chemical Structure

BAY-1143572 Racemate Chemical Structure

CAS No. : 1414943-88-6

Size Price Stock Quantity
1 mg USD 180 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 660 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
25 mg USD 1140 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

BAY 1143572 is a highly selective, potent and orally available inhibitor of PTEFb/CDK9; inhibits the proliferation of AML cell lines with a median IC50 of 385 nM.

IC50 & Target[1] [1]

CDK9

 

In Vitro

BAY 1143572 inhibits the proliferation of 7 MLL-rearrangements positive and negative AML cell lines with a median IC50 of 385 nM (range 230-1100 nM) and induces apoptosis[1]. BAY 1143572 has 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. BAY 1143572 shows a favorable selectivity against a panel of non-CDK kinases. It shows broad antiproliferative activity against a panel of tumor cell lines with sub-micromolar IC50 values. The concentration-dependent inhibition of the phosphorylation of the RNA polymerase II and downstream reduction of MYC mRNA and protein levels is observed[2].

In Vivo

BAY 1143572 exhibits single agent efficacy at tolerated doses in 4 out of 5 AML xenograft tumor models in mice and in 2 out of 2 AML xenograft tumor models in rats upon once daily oral administration. Partial or even complete remissions could be achieved in several models[1].The inhibition of MYC mRNA is also observed in blood cells of BAY 1143572-treated rats indicating the potential clinical utility of MYC in blood cells as a pharmacodynamic marker in clinical development. The in vivo efficacy of BAY 1143572 is significantly enhanced in combination with several chemotherapeutics in different solid tumor models[2].

Clinical Trial
References
Molecular Weight

387.43

Formula

C₁₈H₁₈FN₅O₂S

CAS No.

1414943-88-6

SMILES

N=S(CC1=CC(NC2=NC(C3=CC=C(F)C=C3OC)=NC=N2)=CC=C1)(C)=O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
BAY-1143572 Racemate
Cat. No.:
HY-12871
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