2. Protein Tyrosine Kinase/RTK
  3. VEGFR
  4. Tivozanib hydrate

Tivozanib hydrate  (Synonyms: AV-951 hydrate; KRN951 hydrate)

Cat. No.: HY-112467 Purity: ≥99.0%
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Tivozanib hydrate (AV-951 hydrate; KRN951 hydrate) is the hydrate form of Tivozanib (HY-10977). Tivozanib hydrate is a selective, orally active inhibitor for vascular endothelial growth factor receptor (VEGFR)-1, 2 3, with IC50s of 30, 6.5 and 15 nM, respectively. Tivozanib hydrate exhibits antitumor efficacy.

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

Tivozanib hydrate Chemical Structure

Tivozanib hydrate Chemical Structure

CAS No. : 682745-40-0

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Based on 6 publication(s) in Google Scholar

Other Forms of Tivozanib hydrate:

Tivozanib hydrate 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

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Description

Tivozanib hydrate (AV-951 hydrate; KRN951 hydrate) is the hydrate form of Tivozanib (HY-10977). Tivozanib hydrate is a selective, orally active inhibitor for vascular endothelial growth factor receptor (VEGFR)-1, 2 3, with IC50s of 30, 6.5 and 15 nM, respectively. Tivozanib hydrate exhibits antitumor efficacy[1].

IC50 & Target

VEGFR2

6.5 nM (IC50)

VEGFR3

15 nM (IC50)

VEGFR1

30 nM (IC50)

In Vitro

Tivozanib hydrate inhibits the phosphorylation of VEGFR-1, VEGFR-2, and VEGFR-3, with IC50s of 0.16-0.24 nM[1].
Tivozanib hydrate (0-100 nM, 24 h) inhibits VEGF-induced proliferation of HUVECs with IC50 of 0.67 nM, and migration of HUVECs in dose-dependent manner[1].
Tivozanib hydrate (0-300 nM, 1 h) selectively inhibits the VEGF-stimulated phosphorylation of MAPKs in endothelial cells ligand-dependently, with IC50s of 0.13 and 0.18 nM for ERK1 and ERK2, respectively[1].

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

Tivozanib hydrate Related Antibodies

Cell Proliferation Assay[1]

Cell Line: HUVECs
Concentration: 0-100 nM
Incubation Time: 24 h
Result: Inhibited proliferation.

Cell Migration Assay [1]

Cell Line: HUVECs
Concentration: 0-100 nM
Incubation Time: 22 h
Result: Inhibited migration.

Western Blot Analysis[1]

Cell Line: HUVECs
Concentration: 0-300 nM
Incubation Time: 1 h
Result: Inhibited VEGR-dependent phosphorylation of ERK1 and ERK2.
In Vivo

Tivozanib hydrate (0.04-1 mg/kg, po for 14 days) exhibits antitumor efficacy against breast, colon,hepatic, lung, ovarian, pancreatic, and prostate cancer in model[1].
Tivozanib hydrate (0.2-1 mg/kg, po for 21 days) reversibly suppresses vascular permeability and angiogenesis in Calu-6 tumor bearing rats model[1].
Tivozanib hydrate (5 mg/kg, po, single dose) reveals a AUCinf of 44.5 μg·h/mL, Cmax of 2823 ng/mL in athymic mice model[1].

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

Animal Model: Calu-6 tumor bearing athymic mice model[1]
Dosage: 0.04-1 mg/kg/day
Administration: p.o., for 14-21 days
Result: Inhibited tumor growth, angiogenesis and vascular permeability.
Molecular Weight

472.88

Formula

C22H21ClN4O6
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC=C(C=C1Cl)OC2=CC=NC3=CC(OC)=C(C=C23)OC)NC4=NOC(C)=C4.O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMF : 30 mg/mL (63.44 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1147 mL 10.5735 mL 21.1470 mL
5 mM 0.4229 mL 2.1147 mL 4.2294 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: ≥99.0%

SDS (252 KB)

COA (256 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMF 1 mM 2.1147 mL 10.5735 mL 21.1470 mL 52.8675 mL
5 mM 0.4229 mL 2.1147 mL 4.2294 mL 10.5735 mL
10 mM 0.2115 mL 1.0574 mL 2.1147 mL 5.2868 mL
15 mM 0.1410 mL 0.7049 mL 1.4098 mL 3.5245 mL
20 mM 0.1057 mL 0.5287 mL 1.0574 mL 2.6434 mL
25 mM 0.0846 mL 0.4229 mL 0.8459 mL 2.1147 mL
30 mM 0.0705 mL 0.3525 mL 0.7049 mL 1.7623 mL
40 mM 0.0529 mL 0.2643 mL 0.5287 mL 1.3217 mL
50 mM 0.0423 mL 0.2115 mL 0.4229 mL 1.0574 mL
60 mM 0.0352 mL 0.1762 mL 0.3525 mL 0.8811 mL
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Tivozanib hydrate Related Classifications

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:

Tivozanib682745-40-0AV-951KRN951AV951AV 951KRN 951KRN-951VEGFRVascular endothelial growth factor receptorRCCrenal cell carcinomaC57BL/6 micemacular degenerationHUVECInhibitorinhibitorinhibit

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