A potent Chk1 inhibitor
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CCT245737

Item No. 28775

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-[[4-[[(2R)-2-morpholinylmethyl]amino]-5-(trifluoromethyl)-2-pyridinyl]amino]-2-pyrazinecarbonitrile
CAS Number
1489389-18-5
Molecular Formula
C16H16F3N7O
Formula Weight
379.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
λmax
224, 293, 339 nm
SMILES
FC(F)(F)C(C=N1)=C(NC[C@@H]2OCCNC2)C=C1NC3=CN=C(C#N)C=N3
InChi Code
InChI=1S/C16H16F3N7O/c17-16(18,19)12-8-25-14(26-15-9-22-10(4-20)5-24-15)3-13(12)23-7-11-6-21-1-2-27-11/h3,5,8-9,11,21H,1-2,6-7H2,(H2,23,24,25,26)/t11-/m1/s1
InChi Key
YBYYWUUUGCNAHQ-LLVKDONJSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $119

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    10 mg

    $165

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    Product Description

    CCT245737 is a potent inhibitor of checkpoint kinase 1 (Chk1; IC50 = 1.3 nM).1 It is selective for Chk1 over Chk2 (IC50 = 2,440 nM). CCT245737 inhibits G2 checkpoint arrest induced by etoposide (Item No. 12092) in HT-29 colon cancer cells (IC50 = 30 nM). In vivo, CCT245737 (300 mg/kg) inhibits Chk1 autophosphorylation induced by gemcitabine (Item No. 11690) in an SW620 colon cancer mouse xenograft model. It reduces tumor volume when administered alone or in combination with gemcitabine in an HT-29 mouse xenograft model. CCT245737 (150 mg/kg) reduces inguinal, brachial/axillary, and mesenteric lymph node weights in the Eμ-Myc driven transgenic mouse transplant model of lymph gland-infiltrating B cell lymphoma.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Osborne, J.D., Matthews, T.P., McHardy, T., et al. Multiparameter lead optimization to give an oral checkpoint kinase 1 (CHK1) inhibitor clinical candidate: (R)-5-((4-((morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737). J. Med. Chem. 59(11), 5221-5237 (2016).

    2. Walton, M.I., P.D., E., Hayes, A., et al. The clinical development candidate CCT245737 is an orally active CHK1 inhibitor with preclinical activity in RAS mutant NSCLC and Eµ-MYC driven B-cell lymphoma. Oncotarget 7(3), 2329-2342 (2015).