A Cdk9 inhibitor
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LY2857785

Item No. 34880

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
trans-N1-[4-[2-methyl-3-(1-methylethyl)-2H-indazol-5-yl]-2-pyrimidinyl]-N4-(tetrahydro-2H-pyran-4-yl)-1,4-cyclohexanediamine
CAS Number
1619903-54-6
Molecular Formula
C26H36N6O
Formula Weight
448.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
λmax
227, 258, 264, 342 nm
SMILES
CC(C1=C2C(C=CC(C3=NC(N[C@H]4CC[C@@H](CC4)NC5CCOCC5)=NC=C3)=C2)=NN1C)C
InChi Code
InChI=1S/C26H36N6O/c1-17(2)25-22-16-18(4-9-24(22)31-32(25)3)23-10-13-27-26(30-23)29-20-7-5-19(6-8-20)28-21-11-14-33-15-12-21/h4,9-10,13,16-17,19-21,28H,5-8,11-12,14-15H2,1-3H3,(H,27,29,30)/t19-,20-
InChi Key
LHIUZPIDLZYPRL-MXVIHJGJSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $29

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    5 mg

    $129

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    10 mg

    $229

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    25 mg

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    Product Description

    LY2857785 is an inhibitor of cyclin-dependent kinase 9 (Cdk9; IC50 = 0.011 µM).1 It also inhibits Cdk8 and Cdk7 (IC50s = 0.016 and 0.246 µM, respectively), as well as five kinases in a panel of 114 kinases (IC50s = <0.1 µM for all). LY2857785 inhibits proliferation in a panel of 48 patient-derived solid tumor cell lines, including colon, non-small cell lung, and prostate cancer cells, as well as a panel of 24 hematologic tumor cell lines, including acute lymphoblastic leukemia and multiple myeloma cells, with mean IC50 values of 0.22 and 0.197 µM, respectively. It inhibits phosphorylation of DNA-dependent RNA polymerase II (RNAP II) in peripheral blood mononuclear cells (PBMCs) isolated from patients with acute myeloid leukemia (AML) or chronic lymphocytic leukemia (CLL; IC50s = 0.044 and 0.145 µM, respectively). LY2857785 (3, 6, and 9 mg/kg) reduces tumor growth in an MV4-11 rat xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yin, T., Lallena, M.J., Kreklau, E.L., et al. A novel CDK9 inhibitor shows potent antitumor efficacy in preclinical hematologic tumor models. Mol. Cancer Ther. 13(6), 1442-1456 (2014).