1. Protein Tyrosine Kinase/RTK
    PI3K/Akt/mTOR
    Apoptosis
  2. VEGFR
    PDGFR
    FGFR
    c-Kit
    Akt
    Src
    Apoptosis
  3. Multi-kinase-IN-2

Multi-kinase-IN-2 

Cat. No.: HY-150026
Handling Instructions

Multi-kinase-IN-2 (compound 7h) is an orally active and potent angiokinase inhibitor. Multi-kinase-IN-2 exhibits excellent inhibitory activity against angiokinases including VEGFR-1/2/3, PDGFRα/β, and FGFR-1, as well as LYN and c-KIT kinases. Multi-kinase-IN-2 significantly attenuates phosphorylation of AKT and ERK proteins. Multi-kinase-IN-2 induces cell apoptosis. Multi-kinase-IN-2 shows anticancer activity.

For research use only. We do not sell to patients.

Multi-kinase-IN-2 Chemical Structure

Multi-kinase-IN-2 Chemical Structure

CAS No. : 2095628-21-8

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Description

Multi-kinase-IN-2 (compound 7h) is an orally active and potent angiokinase inhibitor. Multi-kinase-IN-2 exhibits excellent inhibitory activity against angiokinases including VEGFR-1/2/3, PDGFRα/β, and FGFR-1, as well as LYN and c-KIT kinases. Multi-kinase-IN-2 significantly attenuates phosphorylation of AKT and ERK proteins. Multi-kinase-IN-2 induces cell apoptosis. Multi-kinase-IN-2 shows anticancer activity[1].

IC50 & Target

VEGFR-3

6.3 ± 0.5 nM (IC50)

VEGFR-2

6.5 ± 0.9 nM (IC50)

VEGFR-1

31 ± 2.1 nM (IC50)

PDGFRα

7.0 ± 0.1 nM (IC50)

PDGFRβ

9.9 ± 0.7 nM (IC50)

FGFR1

23 ± 2.5 nM (IC50)

pAKT

 

In Vitro

Multi-kinase-IN-2 (compound 7h) (0-10 μM, 14 days) potently inhibits colony formation of HT-29, MKN74, and HepG2 cancer cells[1].
Multi-kinase-IN-2 (0-3 μM, 24 h) significantly attenuates phosphorylation of AKT and ERK proteins[1].
Multi-kinase-IN-2 (0-3 μM, 72 h) induces apoptosis of HT-29, MKN74, and HepG2 cell[1].

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

Cell Proliferation Assay[1]

Cell Line: HT-29, HepG2, and MKN74 cells
Concentration: 0, 0.2, 0.5, 1, and 2 μM or 0, 0.3, 1, 3, and 10 μM
Incubation Time: 14 days
Result: Exhibited excellent activity in inhibition of colony formations in a dose-dependent manner, with remarkable activity at 1 µM concentration.

Western Blot Analysis[1]

Cell Line: HT-29 and HepG2
Concentration: 0, 0.2, 0.5, 1, and 2 μM or 0, 0.3, 1, 3, and 10 μM
Incubation Time: 24 h
Result: Suppressed the phosphorylation of AKT (Ser473) in a dose-dependent manner with a significant inhibition of ERK (Thr202/Tyr204) phosphorylation at 3 μM.

Apoptosis Analysis[1]

Cell Line: HT-29, MKN74, and HepG2 cells
Concentration: 0, 0.3, 1, and 3 μM
Incubation Time: 72 h
Result: Triggered severe apoptosis of HT-29, MKN74, and HepG2 cells in a dose-dependent manner.
In Vivo

Multi-kinase-IN-2 (compound 7h) (100 mg/kg, Orally, once daily for 18 days) displays mild inhibition of tumor growth in mice[1].

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

Animal Model: Female nu/nu mice (4-6 weeks old, HT-29 human colon cancer xenograft model)[1]
Dosage: 100 mg/kg
Administration: Orally, once daily for 18 days
Result: Displayed mild inhibition of tumor growth, with tumor growth inhibition (TGI) value of 13.39%.
Molecular Weight

561.67

Formula

C34H35N5O3

CAS No.
SMILES

O=C(C1=CC(NC/2=O)=C(C=C1)C2=C(NC3=CC=C(N4C(C)=CC=C4CN5CCN(C)CC5)C=C3)/C6=CC=CC=C6)OC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

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Multi-kinase-IN-2
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