An inhibitor of ATR
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SKLB197

Item No. 45728

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-(1H-indol-4-yl)-4-[(3R)-3-methyl-4-morpholinyl]-6-(1methyl-1H-pyrazol-5-yl)-quinazoline
CAS Number
2713577-16-1
Molecular Formula
C25H24N6O
Formula Weight
424.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
C[C@H]1N(CCOC1)C2=NC(C3=C4C=CNC4=CC=C3)=NC5=C2C=C(C6=CC=NN6C)C=C5
InChi Code
InChI=1S/C25H24N6O/c1-16-15-32-13-12-31(16)25-20-14-17(23-9-11-27-30(23)2)6-7-22(20)28-24(29-25)19-4-3-5-21-18(19)8-10-26-21/h3-11,14,16,26H,12-13,15H2,1-2H3/t16-/m1/s1
InChi Key
FCNFJRRMUAOHKI-MRXNPFEDSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $179

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    10 mg

    $340

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    25 mg

    $671

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    50 mg

    $1,074

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    Product Description

    SKLB197 is an inhibitor of ataxia-telangiectasia and Rad3-related protein/kinase (ATR) (IC50 = 0.013 µM).1 It is selective for ATR over a panel of 402 other kinases (IC50s = >1 µM). SKLB197 reduces growth in cancer cell lines deficient in ataxia-telangiectasia mutated kinase (ATM; IC50s = 0.13-0.66 µM) to a greater extent than in ATM-expressing cancer cell lines (IC50s = 3.66-8.79 µM). It induces apoptosis in ATM-deficient LoVo colorectal cancer cells but not in ATM-expressing HT-29 colorectal cancer cells and reduces tumor growth in a LoVo mouse xenograft model when administered at doses of 50 or 100 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bin, H., Chen, P., Wu, M., et al. Discovery of a potent and highly selective inhibitor of ataxia telangiectasia mutated and Rad3-Related (ATR) kinase: Structural activity relationship and antitumor activity both in vitro and in vivo. Eur. J. Med. Chem. 232, 114187 (2022).