SHP2-IN-47
SHP2-IN-47 is a selective and potent SHP2 inhibitor with an IC50 of 0.80 μM. SHP2-IN-47 exhibits potent inhibitory activity against SHP2E76K (IC50 = 0.37 μM). SHP2-IN-47 functionally inhibits protein tyrosine phosphatase domains and downregulates SHP2-mediated phosphorylation of AKT and ERK. SHP2-IN-47 induces apoptosis and suppresses proliferation of cancer cells. SHP2-IN-47 can be used for the research of cancer, such as acute myelocytic leukemia.
For research use only. We do not sell to patients.
- Formula: C34H37Cl2N9O2S2
- Molecular Weight:738.75
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
SHP2-IN-47 (Compound A4) (30 min) potently inhibits recombinant SHP2WT (IC50 = 0.80 μM), SHP2E76K (IC50 = 0.37 μM), and SHP2-PTP catalytic domain (IC50 = 0.32 μM), while displaying no significant inhibition of SHP1 or PTP1B[1].
SHP2-IN-47 (3 days) inhibits the proliferation of MV-4-11 (IC50 = 2.12 μM), KYSE520 (IC50 = 19.82 μM), HCT116 (IC50 = 3.17 μM), MDA-MB-231 (IC50 = 7.71 μM), and HepG2 (IC50 = 4.16 μM) cancer cell lines, and has low toxicity to THP-1-derived macrophages (CC50 > 50 μM)[1].
SHP2-IN-47 (2-6 μM; 24 h) dose-dependently downregulates SHP2-mediated phosphorylation of AKT and ERK in MV-4-11 cells[1].
SHP2-IN-47 (2-6 μM; 24 h) dose-dependently induces apoptosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV-4-11 cells
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Concentration:2, 4, 6 μM
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Incubation Time:24 h
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Result:Reduced the phosphorylation levels of AKT (p-AKT) and ERK (p-ERK) in a dose-dependent manner.
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Cell Line:MV-4-11 cells
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Concentration:2, 4, 6 μM
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Incubation Time:24 h
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Result:Induced apoptosis in a dose-dependent manner, with marked accumulation of cells in the late apoptotic (Annexin V+/PI+) stage.
Chemical Information
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Molecular Weight 738.75
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Formula C34H37Cl2N9O2S2
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SMILES
ClC1=CC(N2C(SC)=NC3=NN(CCCCCNCCCCCN4N=C(N=C(SC)N(C5=CC(Cl)=CC=C5)C6=O)C6=C4)C=C3C2=O)=CC=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SHP2-IN-47 Related Classifications
HY-181800 Related Classifications
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