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

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

Cat. No.: HY-10977A Purity: 99.77%
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Tivozanib hydrochloride hydrate is the hydrate hydrochloride form of Tivozanib (HY-10977). Tivozanib hydrochloride 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 hydrochloride hydrate exhibits antitumor efficacy.

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

Tivozanib hydrochloride hydrate Chemical Structure

Tivozanib hydrochloride hydrate Chemical Structure

CAS No. : 682745-41-1

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Based on 6 publication(s) in Google Scholar

Other Forms of Tivozanib hydrochloride hydrate:

Tivozanib hydrochloride hydrate Related Antibodies

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

  • Biological Activity

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Description

Tivozanib hydrochloride hydrate is the hydrate hydrochloride form of Tivozanib (HY-10977). Tivozanib hydrochloride 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 hydrochloride hydrate exhibits antitumor efficacy[1].

IC50 & Target[3]

VEGFR-2

6.5 nM (IC50)

VEGFR-3

15 nM (IC50)

VEGFR-1

30 nM (IC50)

In Vitro

Tivozanib hydrochloride hydrate inhibits the phosphorylation of VEGFR-1, VEGFR-2, and VEGFR-3, with IC50s of 0.16-0.24 nM[1].
Tivozanib hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride hydrate (0.04-1 mg/kg, po for 14 days) exhibits antitumor efficacy against breast, colon, hepatic, lung, ovarian, pancreatic, and prostate cancer in athymic mice model[1].
Tivozanib hydrochloride 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 hydrochloride 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.
Clinical Trial
Molecular Weight

509.34

Formula

C22H22Cl2N4O6
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.Cl.O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

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

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (245.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9633 mL 9.8166 mL 19.6333 mL
5 mM 0.3927 mL 1.9633 mL 3.9267 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 and light). 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
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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: 99.77%

SDS (393 KB)

COA (258 KB) HNMR (277 KB) LCMS (263 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 and light). 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
DMSO 1 mM 1.9633 mL 9.8166 mL 19.6333 mL 49.0831 mL
5 mM 0.3927 mL 1.9633 mL 3.9267 mL 9.8166 mL
10 mM 0.1963 mL 0.9817 mL 1.9633 mL 4.9083 mL
15 mM 0.1309 mL 0.6544 mL 1.3089 mL 3.2722 mL
20 mM 0.0982 mL 0.4908 mL 0.9817 mL 2.4542 mL
25 mM 0.0785 mL 0.3927 mL 0.7853 mL 1.9633 mL
30 mM 0.0654 mL 0.3272 mL 0.6544 mL 1.6361 mL
40 mM 0.0491 mL 0.2454 mL 0.4908 mL 1.2271 mL
50 mM 0.0393 mL 0.1963 mL 0.3927 mL 0.9817 mL
60 mM 0.0327 mL 0.1636 mL 0.3272 mL 0.8181 mL
80 mM 0.0245 mL 0.1227 mL 0.2454 mL 0.6135 mL
100 mM 0.0196 mL 0.0982 mL 0.1963 mL 0.4908 mL
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Tivozanib hydrochloride 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:

Tivozanib hydrochloride682745-41-1AV-951 hydrochlorideKRN951 hydrochlorideVEGFRVascular endothelial growth factor receptororally activeangiogenesisvascular permeabilityantitumorrenal cell carcinomaInhibitorinhibitorinhibit

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