SHP1-IN-2
SHP1‑IN‑2 is a selective and orally active SHP1 inhibitor. SHP1‑IN‑2 covalently binds to Cys480 of SHP1. SHP1‑IN‑2 elicits potent antitumor immunity and suppresses syngeneic tumor growth. SHP1‑IN‑2 blocks tumor progression in a svngeneic cancer model by activating natural killer cells and cytotoxic CD8＋ T cells, along with reduced T cel l. SHP1‑IN‑2 can be used for cancer‑related research.
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- Formule: C13H10ClN3O3S2
- Masse moléculaire:355.82
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Stockage:
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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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
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ERK1 |
ERK2 |
PLC |
IL-2 |
SHP1-IN-2 (M029) (up to 50 μM; 24-72 h) shows no obvious cytotoxicity in Jurkat T, HEK293, MC38, EO771, B16-F10, and Raw264.7 cells[1].
SHP1-IN-2 (0-20 μM; Anti-CD3 Antibody (OKT-3) (HY-P990864) stimulation for 10 min) enhances the phosphorylation of LCK, PLCγ, and ERK1/2 and promotes IL-2 production in TCR-stimulated Jurkat T cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
SHP1‑IN‑2 (25 mg/kg; once daily) increases infiltration and activation of NK cells and CD8+ T cells, reduces the proportion of PD-1+ TIM3+ exhausted T cells in MC38 tumor tissues, shows no obvious toxicity or body weight loss in tumor‑bearing mice, and loses antitumor efficacy in CD8+ T cell‑depleted mice and nude mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female immunocompetent C57BL/6 mice (6-8 weeks old) are subcutaneously inoculated with MC38 colon cancer cells[1]
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Dosage:25 mg/kg, 100 mg/kg
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Administration:Oral administration; once daily; for 10 days
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Result:Markedly suppresses tumor growth and reduces tumor weight without affecting body weight in mice.
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Animal Model:Female immunocompetent C57BL/6 mice (6-8 weeks old) are subcutaneously inoculated with MC38 colon cancer cells[1]
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Dosage:25 mg/kg
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Administration:Oral administration; once daily; for 10 days
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Result:Significantly increases infiltration and activation of NK cells and CD8+ T cells in tumor tissues.
Reduces the proportion of PD-1+ TIM3+ exhausted T cells in the tumor microenvironment.
Loses antitumor efficacy in CD8+ T cell-depleted mice and nude mice.
Chemical Information
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Masse moléculaire 355.82
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Formule C13H10ClN3O3S2
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SMILES
O=S(C1=CC=C(NC(CCl)=O)C=C1)(NC2=C(C#N)C=CS2)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SHP1-IN-2 Related Classifications
HY-186140 Related Classifications
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