2. Protein Tyrosine Kinase/RTK Stem Cell/Wnt JAK/STAT Signaling Apoptosis PI3K/Akt/mTOR
  3. c-Met/HGFR STAT Apoptosis Akt VEGFR Bcl-2 Family MDM-2/p53 Caspase
  4. 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.

NSC 850745

NSC 850745 Chemical Structure

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NSC 850745 Related Antibodies

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STAT3 STAT5 STAT6 STAT1

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Akt Akt1 Akt2 Akt3

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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Description

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[1].

IC50 & Target[1]

Caspase 3

 

Stat-3

670 nM (IC50)

Akt1

 

Bcl-2

 

Caspase-8

 

Caspase-9

 

c-Met

210 nM (IC50)

In Vitro

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.

NSC 850745 Related Antibodies

RT-PCR[1]

Cell Line: HCT-116
Concentration: 2.41 μM
Incubation Time: 24 and 48 h
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).
Molecular Weight

427.50

Formula

C24H25N7O
SMILES

O=C(CN1CCN(CC1)C2=C3C(N(N=C3)C4=CC=CC=C4)=NC=N2)NCC5=CC=CC=C5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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NSC 850745 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NSC 850745NSC850745NSC-850745c-Met/HGFRSTATApoptosisAktVEGFRBcl-2 FamilyMDM-2/p53CaspasePKBProtein kinase BVascular endothelial growth factor receptorc-MetSTAT3AKT-1VEGFBcl-2p53PUMABaxCyto-Ccaspase-3HT-116Inhibitorinhibitorinhibit

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