A potent Chk1 inhibitor
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CCT244747

Item No. 25666

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[(1R)-2-(dimethylamino)-1-methylethoxy]-5-[[4-methoxy-5-(1-methyl-1H-pyrazol-4-yl)-2-pyridinyl]amino]-2-pyrazinecarbonitrile
CAS Number
1404095-34-6
Molecular Formula
C20H24N8O2
Formula Weight
408.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
SMILES
COC1=C(C2=CN(C)N=C2)C=NC(NC3=CN=C(C#N)C(O[C@H](C)CN(C)C)=N3)=C1
InChi Code
InChI=1S/C20H24N8O2/c1-13(11-27(2)3)30-20-16(7-21)22-10-19(26-20)25-18-6-17(29-5)15(9-23-18)14-8-24-28(4)12-14/h6,8-10,12-13H,11H2,1-5H3,(H,23,25,26)/t13-/m1/s1
InChi Key
IENLGMOXAQMNEH-CYBMUJFWSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $77

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    5 mg

    $228

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    10 mg

    $376

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    Product Description

    CCT244747 is a potent inhibitor of checkpoint kinase 1 (Chk1; IC50 = 8 nM).1 It is selective for Chk1 over FLT3, Chk2, and CDK1 (IC50s = 600, >10,000, and >10,000 nM, respectively) as well as a panel of 121 additional kinases at a concentration of 10 μM. CCT244747 reverses cell cycle arrest at the G2/M phase induced by etoposide (Item No. 12092) and SN-38 (Item No. 15632) in HT-29 cells and gemcitabine (Item Nos. 11690 | 9003096) in SW620 cells, indicating cellular G2 checkpoint abrogation. It potentiates the genotoxicity of SN-38, gemcitabine, and etoposide in HT-29, SW620, MiaPaCa-2, and Calu-6 cells with potentiation index (PI) values ranging from 1.9-8.5, 2.6-12.2, 5-16, and 1.4-5.6, respectively. In vivo, CCT244747 (75 mg/kg), in combination with irinotecan (Item No. 14180) or gemcitabine, increases the delay of tumor growth in SW620 and Calu-6 mouse xenograft models, respectively.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Walton, M.I., Eve, P.D., Hayes, A., et al. CCT244747 is a novel potent and selective CHK1 inhibitor with oral efficacy alone and in combination with genotoxic anticancer drugs. Clin. Cancer Res. 18(20), 5650-5661 (2012).