Multi-kinase-IN-2

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Multi-kinase-IN-2

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CAS NO:

2095628-21-8

Multi-kinase-IN-2 (compound 7h) 是一种口服有效的血管激酶 (angiokinase) 抑制剂。Multi-kinase-IN-2 对血管激酶包括VEGFR-1/2/3,PDGFRα/β和FGFR-1，以及LYN和c-KIT激酶表现出极好的抑制活性。Multi-kinase-IN-2 显著减弱AKT和ERK蛋白的磷酸化。Multi-kinase-IN-2 诱导细胞凋亡 (apoptosis)。Multi-kinase-IN-2 显示抗癌活性。

生物活性

Multi-kinase-IN-2 (compound 7h) is an orally active and potentangiokinaseinhibitor. Multi-kinase-IN-2 exhibits excellent inhibitory activity against angiokinases includingVEGFR-1/2/3,PDGFRα/β, andFGFR-1, as well asLYNandc-KITkinases. Multi-kinase-IN-2 significantly attenuates phosphorylation ofAKTandERKproteins. Multi-kinase-IN-2 induces cellapoptosis. 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)

体外研究
(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].

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.

体内研究
(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].

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%.

分子量

561.67

Formula

C₃₄H₃₅N₅O₃

CAS 号

2095628-21-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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