SHP2-IN-46
SHP2-IN-46 is an orally active SHP2 inhibitor (IC50 = 11.76 μM). SHP2-IN-46 inhibits SHP2 enzymatic activity and mediates anti-tumor activity. SHP2-IN-46 suppresses cell proliferation in various cancer cells. SHP2-IN-46 can be used in research related to lung adenocarcinoma, pancreatic cancer and hepatoblastoma.
For research use only. We do not sell to patients.
- CAS No.: 3086360-36-0
- Formula: C17H19N5O
- Molecular Weight:309.37
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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-46 (72 h) potently inhibits the proliferation of A549, MIA PaCa-2, and HepG2 cancer cells with IC50 values of 0.24 μM, 0.16 μM, and 0.09 μM, respectively[1].
SHP2-IN-46 (24 h) induces S-phase cell cycle arrest in HepG2 cells, disrupting cell proliferation[1].
SHP2-IN-46 (up to 60 min) shows favorable metabolic stability in human liver microsomes, with an in vitro T1/2 of 40.63 min and CLint of 34.11 μL/min/mg protein[1].
SHP2-IN-46 (0.001-100 μM; 60 min enzyme incubation; 30 min substrate incubation) inhibits SHP2 enzyme activity with an IC50 value of 11.76 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HePG2 cells
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Concentration:0.5 μM
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Incubation Time:24 h
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Result:Promoted the transition from G1 to S phase and subsequently induce S-phase arrest.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR mice (8 weeks old, 50% male/female)[1]
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Dosage:50 mg/kg; 100 mg/kg; 200 mg/kg
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Administration:p.o.; single dose
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Result:Had a maximum tolerated dose greater than 200 mg/kg in ICR mice.
Chemical Information
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CAS No. 3086360-36-0
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Molecular Weight 309.37
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Formula C17H19N5O
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SMILES
CC(C=C1NC2=CC=CC=C2C)=NN1C(N3)=NC(C)=C(C)C3=O
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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)
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