A PI3Kδ inhibitor
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GS-9901

Item No. 42105

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2,4-diamino-6-[[(S)-[5-chloro-8-fluoro-3,4-dihydro-4-oxo-3-(3-pyridinyl)-2-quinazolinyl]cyclopropylmethyl]amino]-5-pyrimidinecarbonitrile
CAS Number
1640247-87-5
Molecular Formula
C22H17ClFN9O
Formula Weight
477.9
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlMethanol: Sparingly soluble: 1-10 mg/ml
SMILES
N#CC(C(N[C@@H](C1CC1)C(N(C2=CN=CC=C2)C(C3=C(Cl)C=C4)=O)=NC3=C4F)=NC(N)=N5)=C5N
InChi Code
InChI=1S/C22H17ClFN9O/c23-13-5-6-14(24)17-15(13)21(34)33(11-2-1-7-28-9-11)20(30-17)16(10-3-4-10)29-19-12(8-25)18(26)31-22(27)32-19/h1-2,5-7,9-10,16H,3-4H2,(H5,26,27,29,31,32)/t16-/m0/s1
InChi Key
XDSXYMOZKDUASY-INIZCTEOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $87

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    5 mg

    $239

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    10 mg

    $435

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    Product Description

    GS-9901 is an inhibitor of PI3Kδ (IC50 = 1 nM).1 It is selective for PI3Kδ over PI3Kα, PI3Kβ, and PI3Kγ (IC50s = 750, 100, and 190 nM, respectively) and a panel of 456 additional kinases, including 11 lipid and 56 mutant kinases, at 10 µM. GS-9901 activates basophils in isolated human whole blood (EC50 = 1 nM). In vivo, GS-9901 (1 and 3 mg/kg) decreases ankle swelling and disease severity in a rat model of collagen-induced arthritis.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Patel, L., Chandrasekhar, J., Evarts, J., et al. Discovery of orally efficacious phosphoinositide 3-kinase δ inhibitors with improved metabolic stability. J. Med. Chem. 59(19), 9228-9242 (2016).