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

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。

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Multi-kinase-IN-2 Chemical Structure

Multi-kinase-IN-2 Chemical Structure

CAS No. : 2095628-21-8

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Multi-kinase-IN-2 相关抗体

Top Publications Citing Use of Products

查看 VEGFR 亚型特异性产品:

查看所有亚型
VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

查看 PDGFR 亚型特异性产品:

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PDGFR PDGFRβ PDGFRα

查看 FGFR 亚型特异性产品:

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FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

查看 Akt 亚型特异性产品:

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Akt Akt1 Akt2 Akt3

查看 Src 亚型特异性产品:

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Lck Fyn Blk

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Sf9 IC50
7 nM
Compound: 7h
Inhibition of N-terminal GST-tagged human recombinant PDGFRalpha D842I mutant expressed in baculovirus-infected Sf9 cells using FAM-labeled peptide and ATP as substrate preincubated for 10 mins followed by substrate addition measured after 1 hr by mobilit
Inhibition of N-terminal GST-tagged human recombinant PDGFRalpha D842I mutant expressed in baculovirus-infected Sf9 cells using FAM-labeled peptide and ATP as substrate preincubated for 10 mins followed by substrate addition measured after 1 hr by mobilit
[PMID: 32305182]
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].

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

Multi-kinase-IN-2 相关抗体:

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].

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%.
分子量

561.67

Formula

C34H35N5O3
CAS 号
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.
纯度 & 产品资料
参考文献

Multi-kinase-IN-2 相关分类

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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:

Multi-kinase-IN-22095628-21-8VEGFRPDGFRFGFRc-KitAktSrcApoptosisVascular endothelial growth factor receptorPlatelet-derived growth factor receptorFibroblast growth factor receptorSCFRCD117PKBProtein kinase BMulti-kinase inhibitorAntitumor activityangiokinaseHT-29MKN74HepG2Inhibitorinhibitorinhibit

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