A selective checkpoint kinase inhibitor
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AZD 7762

Item No. 11491

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[(aminocarbonyl)amino]-5-(3-fluorophenyl)-N-(3S)-3-piperidinyl-2-thiophenecarboxamide
CAS Number
860352-01-8
Molecular Formula
C17H19FN4O2S
Formula Weight
362.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 10 mg/mlEthanol: 10 mg/mlPBS (pH 7.2): 10 mg/ml
λmax
251, 303 nm
SMILES
O=C(N[C@@H]1CNCCC1)C2=C(NC(N)=O)C=C(C3=CC=CC(F)=C3)S2
InChi Code
InChI=1S/C17H19FN4O2S/c18-11-4-1-3-10(7-11)14-8-13(22-17(19)24)15(25-14)16(23)21-12-5-2-6-20-9-12/h1,3-4,7-8,12,20H,2,5-6,9H2,(H,21,23)(H3,19,22,24)/t12-/m0/s1
InChi Key
IAYGCINLNONXHY-LBPRGKRZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $28

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    5 mg

    $62

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    10 mg

    $97

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    25 mg

    $172

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    Product Description

    AZD 7762 selectively inhibits the activity of checkpoint kinases (Chk) 1 and Chk2 (IC50s = 5 nM) by competitively and reversibly binding their respective ATP-binding sites (Ki = 3.6 nM for Chk1).1 AZD 7762 abrogates DNA damage-induced S and G2 checkpoints with an EC50 value of 10 nM and potentiates the efficacy of DNA-damage repair prohibitive agents, gemcitabine and topotecan, both in vitro and in various tumor xenografts by modulating downstream checkpoint pathway proteins.1,2,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zabludoff, S.D., Deng, C., Grondine, M.R., et al. AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies. Mol. Cancer Ther. 7, 2955-2966 (2008).

    2. Mitchell, J.B., Choudhuri, R., Fabre, K., et al. In vitro and in vivo radiation sensitization of human tumor cells by a novel checkpoint kinase inhibitor, AZD7762. Clin. Cancer Res. 16(7), 2076-2084 (2010).

    3. Morgan, M.A., Parsels, L.A., Zhao, L., et al. Mechanism of radiosensitization by the Chk1/2 inhibitor AZD7762 involves abrogation of the G2 checkpoint and inhibition of homologous recombinational DNA repair. Cancer Res. 70(12), 4972-4981 (2010).