2. Protein Tyrosine Kinase/RTK Epigenetics Cell Cycle/DNA Damage Cytoskeleton
  3. VEGFR HDAC Microtubule/Tubulin
  4. 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.

VEGFR2/HDAC-IN-1

VEGFR2/HDAC-IN-1 Chemical Structure

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VEGFR2/HDAC-IN-1 Related Antibodies

Top Publications Citing Use of Products

View All VEGFR Isoform Specific Products:

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

View All HDAC Isoform Specific Products:

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

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Description

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[1].

IC50 & Target[1]

VEGFR2

19.19 nM (IC50)

HDAC6

0.165 μM (IC50)

HDAC1

1.830 μM (IC50)

In Vitro

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.

VEGFR2/HDAC-IN-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: HUVEC, HeLa
Concentration: 0.1, 0.5, 1.0 μM (HUVECs); 0.5, 1.0, 10 μM (HeLa cells)
Incubation Time: 24 h
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.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-t MRT0-t Bioavailability Vss_obs CL_obs
Rat[1] 3 mg/kg i.v. 3.08 h / / 3204.81 ng·h/mL 1.72 h / 1638.43 mL/kg 934.80 mL/h/kg
Rat[1] 15 mg/kg p.o. 4.37 h 0.50 h 620.00 ng/mL 3160.00 mL/h/kg 4.44 h 19.72 % / /
In Vivo

VEGFR2/HDAC-IN-1 (10i) (50 mg/kg; p.o.; daily; 16 consecutive days) produces a 64.4% tumor growth inhibition in HT-29 xenograft mice with a favorable safety profile[1].
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.

Animal Model: BALB/c nude (male, 5-week-old, 18-20 g, subcutaneous inoculation of HT-29 cells)[1]
Dosage: 50 mg/kg
Administration: p.o.; daily; 16 consecutive days
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.
Animal Model: BALB/c nude (male, 5-week-old, 18-20 g, subcutaneous inoculation of HCCLM3/Sorafenib cells)[1]
Dosage: 50 mg/kg
Administration: p.o.; daily; 16 consecutive days
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.
Molecular Weight

542.46

Formula

C26H21F3N4O6
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
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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VEGFR2/HDAC-IN-1 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:

VEGFR2/HDAC-IN-1VEGFRHDACMicrotubule/TubulinVascular endothelial growth factor receptorHistone deacetylasesHDAC6colorectal carcinomaHDAC1A549 cellsHDAC8HeLa cellsVEGFR2HUVECsHT-29 cellshepatocellular carcinomaInhibitorinhibitorinhibit

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