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.
For research use only. We do not sell to patients.
- Formula: C24H25N7O
- Molecular Weight:427.50
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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
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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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Molecular Weight 427.50
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Formula 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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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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