2. Protein Tyrosine Kinase/RTK Apoptosis
  3. c-Met/HGFR Apoptosis
  4. c-Met-IN-22

c-Met-IN-22 (compound 51am) is an orally active inhibitor against c-Met with an IC50 value of 2.54 nM. c-Met-IN-22 has antiproliferative and antitumor activities. c-Met-IN-22 induces cell apoptosis.

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c-Met-IN-22 Chemical Structure

c-Met-IN-22 Chemical Structure

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c-Met-IN-22 Related Antibodies

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Description

c-Met-IN-22 (compound 51am) is an orally active inhibitor against c-Met with an IC50 value of 2.54 nM. c-Met-IN-22 has antiproliferative and antitumor activities. c-Met-IN-22 induces cell apoptosis[1].

IC50 & Target[1]

c-Metwild type

2.54 nM (IC50)

c-MetH1094R

93.6 nM (IC50)

c-MetD1228H

29.4 nM (IC50)

c-MetY1230H

45.8 nM (IC50)

c-MetY1235D

54.2 nM (IC50)

c-MetM1250T

26.5 nM (IC50)

c-Metkit

4.94 nM (IC50)

c-MetRon

3.83 nM (IC50)

c-MetPDGFRα

425 nM (IC50)

c-MetPDGFRβ

513 nM (IC50)

c-MetVEGFR-2

527 nM (IC50)

c-MetFit-3

6.12 nM (IC50)

c-MetFit-4

276 nM (IC50)

In Vitro

c-Met-IN-22 shows antiproliferative activity against MKN-45, A-549, HT-29, MDA-MB-231, HUVEC and FHC with IC50s of 0.092, 0.83, 0.68, 3.94,2.54 and 8.63 μM, respectively[1].
c-Met-IN-22 shows anti-drug resistence against tH1094R, D1228H, Y1230H, Y1235D, and M1250T, with IC50 values of 93.6, 29.4, 45.8, 54.2 and 26.5 nM,respectively[1].
c-Met-IN-22 (0, 2.5, 5.0, and 10.0 μM, 24 h) inhibits c-Met phosphorylation in MKN-45 in a dose-dependent manner[1] .
c-Met-IN-22 (0.4, 0.8, and 1.2  μM, 24 h) induces cell cycle arrest at G2 phase and apotosis of MNK-45 in a dose-dependent manner[1].

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

c-Met-IN-22 Related Antibodies

Apoptosis Analysis[1]

Cell Line: MNK- 45 cells
Concentration: 0.4, 0.8, 1.2 μM
Incubation Time: 24 h
Result: Induced cell apoptosis in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: MNK- 45 cells
Concentration: 0.4, 0.8, 1.2 μM
Incubation Time: 24 h
Result: Induced cell cycle arrest at G2 phase in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: MNK- 45 cells
Concentration: 0, 2.5, 5, 10 μM
Incubation Time: 24 h
Result: Inhibited c-Met phosphorylation in a dose-dependent manner.
In Vivo

c-Met-IN-22 (10mg/kg;p.o.;single dose) exhibits good oral bioavailability (F=69%) in BALB/c mice, with elimination half-time of 5.6h and clearance of 0.87 L/h•kg[1].
c-Met-IN-22 (1.5mg/kg;i.v.) exhibits an elimination half-time of 3.2h[1].

Pharmacokinetic Analysis of c-Met-IN-22 in BALB/c mice[1]

Route Dose (mg/kg) AUC0→∞ (μg·h/mL) T1/2 (h) Tmax (h) Cmax (ng/mL) Cl (L/h·kg) F (%)
i.v. 1.5mg/kg 2.5 3.2 / 552 0.6 /
p.o. 10mg/kg 11.5 5.6 4.1 1756 / 69

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

Animal Model: Pharmacokinetic Analysis in BALB/c mice
Dosage: p.o.10 mg/kg; i.v. 1.5 mg/kg
Administration: Intravenous (i.v.) injection, Oral administration (p.o.)
Result: Characterised good maximum concentration, plasma exposure and elimination half-time in pharmacokinetics.
Molecular Weight

512.74

Formula

C21H10Cl3F2N3O2S
SMILES

O=C(C1=NC(C2=CC=C(F)C(Cl)=C2)=CS1)NC3=CC=C(OC4=C(Cl)C(Cl)=NC=C4)C(F)=C3
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-22 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-22c-Met/HGFRApoptosisc-MetBALB/c mice MNK-45A-549HT-29MDA-MB-231HUVECFHCInhibitorinhibitorinhibit

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