An orally bioavailable inhibitor of SHP2
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SHP099

Item No. 20000

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-(4-amino-4-methyl-1-piperidinyl)-3-(2,3-dichlorophenyl)-2-pyrazinamine
CAS Number
1801747-42-1
Molecular Formula
C16H19Cl2N5
Formula Weight
352.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS(pH 7.2) (1:2): 0.33 mg/mlEthanol: 10 mg/ml
λmax
247, 351 nm
SMILES
ClC1=C(Cl)C(C2=NC=C(N3CCC(C)(N)CC3)N=C2N)=CC=C1
InChi Code
InChI=1S/C16H19Cl2N5/c1-16(20)5-7-23(8-6-16)12-9-21-14(15(19)22-12)10-3-2-4-11(17)13(10)18/h2-4,9H,5-8,20H2,1H3,(H2,19,22)
InChi Key
YGUFCDOEKKVKJK-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    500 µg

    $49

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    1 mg

    $93

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    5 mg

    $423

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    10 mg

    $748

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    Cayman Chemical
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    Product Description

    SHP099 is an orally bioavailable inhibitor of SHP2, a non-receptor protein tyrosine phosphatase (IC50 = 71 nM).1,2 It stabilizes SHP2 in an auto-inhibited conformation.2 SHP099 suppresses signaling through the Ras-ERK pathway and blocks the proliferation of receptor tyrosine kinase-driven human cancer cells in vitro and in vivo.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Garcia Fortanet, J., Chen, C.H.-T., Chen, Y.-N.P., et al. Allosteric inhibition of SHP2: Identification of a potent, selective, and orally efficacious phosphatase inhibitor. J. Med. Chem. 59(17), 7773-7782 (2016).

    2. Chen, Y.-N.P., LaMarche, M.J., Chan, H.M., et al. Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases. Nature 535(7610), 148-152 (2016).