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Cat. No.: HY-150582

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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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CAS No.: 2443380-34-3
Formule: C₃₄H₃₈ClFN₄O₇S
Masse moléculaire:701.20

Stockage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (283 KB)

c-Met-IN-14 Chemical Structure

CAS No.: 2443380-34-3

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

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.

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 (T_max=2.5 h), high maximum concentration (C_max=1228.4 ng/mL), high plasma exposure (AUC_0-∞=6.8 µg.h.mL^-1), accepted elimination half-life (T_1/2=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) T_1/2 (h) C_max (ng.mL^-1) T_max (h) AUC_0-∞ (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

Related Protocols :

Chemical Information

CAS No. 2443380-34-3
Masse moléculaire 701.20
Formule C₃₄H₃₈ClFN₄O₇S
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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (283 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Nan X, et al. Design, synthesis and biological evaluation of novel N-sulfonylamidine-based derivatives as c-Met inhibitors via Cu-catalyzed three-component reaction. Eur J Med Chem. 2020 Aug 15. 200:112470. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références

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c-Met-IN-14