A Chk1 inhibitor
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GDC-0575

Item No. 34300

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-[(3R)-3-amino-1-piperidinyl]-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl]-cyclopropanecarboxamide
CAS Number
1196541-47-5
Molecular Formula
C16H20BrN5O
Formula Weight
378.3
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:5): 0.16 mg/mlEthanol: 1 mg/ml
λmax
251 nm
SMILES
O=C(C1CC1)NC2=CNC3=NC=C(Br)C(N4C[C@@H](CCC4)N)=C23
InChi Code
InChI=1S/C16H20BrN5O/c17-11-6-19-15-13(14(11)22-5-1-2-10(18)8-22)12(7-20-15)21-16(23)9-3-4-9/h6-7,9-10H,1-5,8,18H2,(H,19,20)(H,21,23)/t10-/m1/s1
InChi Key
BAZRWWGASYWYGB-SNVBAGLBSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

    $303

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    25 mg

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    Product Description

    GDC-0575 is an inhibitor of checkpoint kinase 1 (Chk1; IC50 = 1.2 nM).1 It is greater than 30-fold selective for Chk1 over a panel of more than 450 wild-type and mutant kinases. GDC-0575 (500 nM) enhances apoptosis induced by cytarabine (Item No. 16069) in HL-60, KG-1, U937, and ML-1 human acute myeloid leukemia (AML) cells. It nearly completely eliminates tumor burden in AML patient-derived xenograft (PDX) mouse models when administered at a dose of 7.5 mg/kg in combination with cytarabine.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Di Tullio, A., Rouault-Pierre, K., Abarrategi, A., et al. The combination of CHK1 inhibitor with G-CSF overrides cytarabine resistance in human acute myeloid leukemia. Nat. Commun. 8(1), 1679 (2017).