VEGFR2/HDAC-IN-1
VEGFR2/HDAC-IN-1 is a dual selective enzymatic inhibitor of VEGFR2 kinase and HDAC6 with oral activity. VEGFR2/HDAC-IN-1 has an IC50 of 19.19 nM for VEGFR2 and 0.165 μM for HDAC6. VEGFR2/HDAC-IN-1 increases α-tubulin acetylation, exerts antiproliferative effects, inhibits tumor growth, and exhibits antiangiogenic activity. VEGFR2/HDAC-IN-1 can be used for the research of colorectal carcinoma and hepatocellular carcinoma.
For research use only. We do not sell to patients.
- Formula: C26H21F3N4O6
- Molecular Weight:542.46
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All VEGFR Isoforms
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Biological Activity
|
VEGFR2 19.19 nM (IC50) |
HDAC6 0.165 μM (IC50) |
HDAC1 1.830 μM (IC50) |
VEGFR2/HDAC-IN-1 (10i) potently inhibits purified VEGFR2 kinase with an IC50 of 19.19 nM[1].
VEGFR2/HDAC-IN-1 inhibits HDAC activity with isoform selectivity, showing the highest potency against HDAC6 (IC50 = 0.165 μM), moderate activity against HDAC1 (IC50 = 1.830 μM), and no significant activity against HDAC8, while inhibiting 61% of HDAC activity in HeLa nuclear extracts[1].
VEGFR2/HDAC-IN-1 (72 h) potently inhibits proliferation of multiple cancer cell lines (A549, HT-29, HeLa) and HUVECs, with lower activity against normal HEK-293T cells, showing highest potency against A549 cells (IC50 = 0.24 μM)[1].
VEGFR2/HDAC-IN-1 (0.1-10.0 μM; 24 h) inhibits VEGFR2 phosphorylation in a dose-dependent manner in HUVECs (complete inhibition at 1.0 μM) and increases HDAC6 substrate acetylation (acetylated α-tubulin) in a dose-dependent manner in HeLa cells, confirming intracellular target inhibition[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HUVEC, HeLa
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Concentration:0.1, 0.5, 1.0 μM (HUVECs); 0.5, 1.0, 10 μM (HeLa cells)
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Incubation Time:24 h
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Result:Caused a dose-dependent decrease in p-VEGFR2 levels in HUVECs, with complete inhibition at 1.0 μM.
Caused a dose-dependent increase in acetylated α-tubulin levels in HeLa cells, with a marked increase at 10.0 μM.
VEGFR2/HDAC-IN-1 (50 mg/kg; p.o.; daily; 16 consecutive days) produces an 89.72% tumor growth inhibition in Sorafenib (HY-10201)-resistant HCCLM3/Sorafenib xenograft mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (male, 5-week-old, 18-20 g, subcutaneous inoculation of HT-29 cells)[1]
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Dosage:50 mg/kg
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Administration:p.o.; daily; 16 consecutive days
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Result:Achieved a tumor growth inhibition (TGI) of 64.4%.
Caused no significant body weight loss during treatment.
Detected no tumor metastasis in treated mice.
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Animal Model:BALB/c nude (male, 5-week-old, 18-20 g, subcutaneous inoculation of HCCLM3/Sorafenib cells)[1]
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Dosage:50 mg/kg
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Administration:p.o.; daily; 16 consecutive days
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Result:Achieved a tumor growth inhibition (TGI) of 89.72%, which was higher than the TGI of SAHA monotherapy, sorafenib monotherapy, and the SAHA-sorafenib combination.
Caused no significant body weight loss during treatment.
Chemical Information
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Molecular Weight 542.46
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Formula C26H21F3N4O6
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SMILES
COC1=C(C=C(C2=C1)N=CC=C2OC3=CC(C(F)(F)F)=C(C=C3)NC(NC4=CC=C(C=C4)C(NO)=O)=O)OC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
VEGFR2/HDAC-IN-1 Related Classifications
HY-181793 Related Classifications
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