1. Cell Cycle/DNA Damage
  2. CDK

Atuveciclib Racemate (Synonyms: BAY-1143572 Racemate)

Cat. No.: HY-12871 Purity: 98.48%
Handling Instructions

Atuveciclib Racemate (BAY-1143572 Racemate) is the racemate mixture of Atuveciclib. Atuveciclib is a potent and highly selective, oral P-TEFb/CDK9 inhibitor which supresses CDK9/CycT1 with an IC50 of 13 nM.

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

Atuveciclib Racemate Chemical Structure

Atuveciclib Racemate Chemical Structure

CAS No. : 1414943-88-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 358 In-stock
Estimated Time of Arrival: December 31
1 mg USD 180 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 660 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1140 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Other Forms of Atuveciclib Racemate:

Top Publications Citing Use of Products

    Atuveciclib Racemate purchased from MCE. Usage Cited in: Haematologica. 2018 Jul;103(7):1110-1123.

    Treat c-Kit+ BM cells from Setd2f/f/Vav1-Cre mice with JQ1 500nM, EPZ-5676 1uM, BAY 1143572 400nM for 24 hours. Then cells are collected to determined the proteins levels of H3K36me1/2, H3K4me3, H3K79me2, H3K27me3, H3, RNA pol II (Ser2P), pol II (Ser5P), Gata1, Gata3, Myc, and β-actin by immunoblotting.
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    Description

    Atuveciclib Racemate (BAY-1143572 Racemate) is the racemate mixture of Atuveciclib. Atuveciclib is a potent and highly selective, oral P-TEFb/CDK9 inhibitor which supresses CDK9/CycT1 with an IC50 of 13 nM.

    IC50 & Target

    CDK9

     

    In Vitro

    Atuveciclib (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]. Atuveciclib (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. Atuveciclib (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

    Atuveciclib (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 Atuveciclib (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 Atuveciclib (BAY-1143572) is significantly enhanced in combination with several chemotherapeutics in different solid tumor models[2].

    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

    Purity: 98.48%

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    Product Name:
    Atuveciclib Racemate
    Cat. No.:
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    Atuveciclib Racemate

    Cat. No.: HY-12871