NSC 850745
NSC 850745 is a selective and potent c-Met/STAT3 inhibitor with IC50 values of 210 and 670 nM. NSC 850745 can inhibit cell proliferation, induce G2/M phase arrest and induce apoptosis. NSC 850745 can downregulate AKT-1, VEGF and Bcl-2 expression and upregulate p53, Bax and caspase expression. NSC 850745 can be used for the research of cancer, such as leukemia and colon cancer.
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- Formule: C24H25N7O
- Masse moléculaire:427.50
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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
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Activité biologique
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Caspase 3 |
Stat-3 670 nM (IC50) |
Akt1 |
Bcl-2 |
Caspase-8 |
Caspase-9 |
c-Met 210 nM (IC50) |
NSC 850745 (Compound 22b) exhibits subpanel mean GI50, TGI, and LC50 of 6.97, 17.15, and 43.56 μM for leukemia cells.[1].
NSC 850745 displays the strongest potency against EKVX (non-small cell lung cancer) and CAKI-1 (renal cancer) cells (GI50 = 1.1, 1.17 μM) [1].
NSC 850745 (10 μM) achieves 96.9% and 95.7% phosphorylation inhibition for c-Met and STAT3[1].
NSC 850745 inhibits HCT-116 colon cancer cells with an IC50 of 2.41 μM and shows an IC50 of 56.25 μM against normal WI-38 fibroblasts with a selectivity index of 23.3[1].
NSC 850745 (2.41 μM, 24 h) induces G2/M phase arrest and triggers late apoptosis and necrosis in HCT-116 cells[1].
NSC 850745 (2.41 μM, 24-48 h) downregulates AKT-1, VEGF, Bcl-2 gene expression and regulates p53, PUMA, Bax, Cyto-C, caspase-3, caspase-8 and caspase-9 expression in HCT-116 cells[1].
NSC 850745 (2.41 μM, 24 h) reduces ATPase activity in HCT-116 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT-116
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Concentration:2.41 μM
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Incubation Time:24 and 48 h
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Result:Downregulated AKT-1 (0.59-fold) and VEGF (0.07-fold) genes.
Upregulated p53 (4.74-fold), PUMA (4.99-fold), Bax (3.43-fold), and Cyto-C (4.89-fold) .
Downregulated Bcl-2 (0.44-fold) with a Bax/Bcl-2 ratio of 7.79-fold.
Activated caspase-3 (6.1-fold), -8 (1.9-fold), and -9 (5.5-fold).
Chemical Information
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Masse moléculaire 427.50
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Formule C24H25N7O
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SMILES
O=C(CN1CCN(CC1)C2=C3C(N(N=C3)C4=CC=CC=C4)=NC=N2)NCC5=CC=CC=C5
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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)
NSC 850745 Related Classifications
HY-175848 Related Classifications
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