2. Protein Tyrosine Kinase/RTK Apoptosis
  3. c-Met/HGFR c-Kit FLT3 Apoptosis
  4. c-Met-IN-14

c-Met-IN-14 (compound 26af) is a selective inhibitor of c-Met kinase from N-sulfonylamidine-based derivatives, with an IC50 value of 2.89 nM. c-Met-IN-14 shows anticancer activity by blocking phosphorylation of c-Met, and arrests cell cycle at G2/M phase. c-Met-IN-14 induces apoptosis of A549 cells in a dose-dependent manner.

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c-Met-IN-14

c-Met-IN-14 Chemical Structure

CAS No. : 2443380-34-3

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c-Met-IN-14 Related Antibodies

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Description

c-Met-IN-14 (compound 26af) is a selective inhibitor of c-Met kinase from N-sulfonylamidine-based derivatives, with an IC50 value of 2.89 nM. c-Met-IN-14 shows anticancer activity by blocking phosphorylation of c-Met, and arrests cell cycle at G2/M phase. c-Met-IN-14 induces apoptosis of A549 cells in a dose-dependent manner[1].

IC50 & Target

IC50: 2.89 nM (c-Met); 4.26 nM (c-kit); 7.28 nM (Flt-3)[1]
Cellular Effect
Cell Line Type Value Description References
A549 IC50
0.28 μM
Compound: 26af
Cytotoxicity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
[PMID: 32505087]
FHC IC50
6.12 μM
Compound: 26af
Cytotoxicity against human FHC cells assessed as inhibtion of cell proliferation measured after 72 hrs by MTT assay
Cytotoxicity against human FHC cells assessed as inhibtion of cell proliferation measured after 72 hrs by MTT assay
[PMID: 32505087]
HT-29 IC50
0.32 μM
Compound: 26af
Cytotoxicity against human HT-29 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Cytotoxicity against human HT-29 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
[PMID: 32505087]
HUVEC IC50
1.35 μM
Compound: 26af
Cytotoxicity against human HUVEC cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Cytotoxicity against human HUVEC cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
[PMID: 32505087]
MDA-MB-231 IC50
0.72 μM
Compound: 26af
Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
[PMID: 32505087]
MKN-45 IC50
0.48 μM
Compound: 26af
Cytotoxicity against human MKN-45 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Cytotoxicity against human MKN-45 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
[PMID: 32505087]
In Vitro

c-Met-IN-14 (compound 26af) is a relatively selective inhibitor of c-Met kinase (IC50=2.89 nM), because of high inhibitory effects against c-Kit (IC50=4.26 nM) and Flt-3 (IC50=7.28 nM)[1].
c-Met-IN-14 (0.28-0.72 μM; 24 h) exhibits the remarkable anti-proliferative activities against cancer cell lines (A549, HT-29, MKN-45 and MDA-MB-231), with IC50s of 0.28-0.72 μM[1].
c-Met-IN-14 (0.25, 0.5, and 1.0 μM; 12 h) induces the late apoptotic and early apoptotic and (0.25, 0.5, and 1.0 μM; 24 h) shows anti-proliferative of A549 cells by arresting cell cycle at G2/M phase and apoptosis induction[1].
c-Met-IN-14 (1.35, or 6.12 μM, respectively; 24 h) has moderate selectivity towards cancer cells over normal cells, with the selectivity index of 4.2 and 19.1 to HUVEC (IC50=1.35 μM) and FHC cells (IC50=6.12 μM), respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

c-Met-IN-14 Related Antibodies

Western Blot Analysis[1]

Cell Line: A549
Concentration: 0, 2, 4, 8 μM
Incubation Time: 6 hours
Result: Showed excellent inhibition against c-Met phosphorylation in a concentration-dependent manner.
In Vivo

c-Met-IN-14 (compound 26af) (p.o.; 8 mg/kg) exhibits safety profile and favorable pharmacokinetic properties in BALB/c mouse, with rapid absorption (Tmax=2.5 h), high maximum concentration (Cmax=1228.4 ng/mL), high plasma exposure (AUC0-∞=6.8 µg.h.mL-1), accepted elimination half-life (T1/2=3.5 h), and well clearance (1.18 L.h-1.kg-1), has a moderate oral bioavailability (74%) in mouse[1].
c-Met-IN-14 (i.p.; below 200 mg/kg) doesn’t cause abnormalities, anaphylactic responses, allergic reactions on mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 8-week-old male BALB/c mice [1]
Dosage: 0 (vehicle), 100, 200, 300, or 400 mg/kg
Administration: Intraperitoneal injection; treatment on day 0 and assessment every 3 days for 15 days
Result: Showed no obvious toxicity in acute toxicity tests.
Animal Model: Pharmacokinetic profiles of compound 26af in BALB/c mouse[1]
Dosage:
Administration:
Result:
Route Dose (mg/kg) T1/2 (h) Cmax (ng.mL-1) Tmax (h) AUC0-∞ (μg.h.mL-1) CL (L.h-1.kg-1) CL (%)
i.v. 2 1.8 675.6 - 2.3 -
p.o. 8 3.5 1228.4 2.5 6.8 1.18 74
Molecular Weight

701.20

Formula

C34H38ClFN4O7S
CAS No.
SMILES

COCC/C(NC1=CC=C(OC2=CC=NC3=CC(OCCCN4CCOCC4)=C(OC)C=C23)C(F)=C1)=N/S(=O)(CC5=CC=C(Cl)C=C5)=O
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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c-Met-IN-14 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:

c-Met-IN-142443380-34-3c-Met/HGFRc-KitFLT3ApoptosisSCFRCD117Cluster of differentiation antigen 135CD135Fms like tyrosine kinase 3N-Sulfonylamidineanticancer activityapoptosisc-Met phosphorylationG2/M arrestpharmacokineticrelatively selectivec-kitc-MetFlt-3A549 cellsInhibitorinhibitorinhibit

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