2. Protein Tyrosine Kinase/RTK
  3. VEGFR PDGFR c-Kit
  4. Telatinib mesylate

Telatinib mesylate  (Synonyms: Bay 57-9352 mesylate)

Cat. No.: HY-10527C Purity: 99.74%
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Telatinib mesylate (Bay 57-9352 mesylate) is a potent and orally active VEGFR2, VEGFR3, PDGFα, and c-Kit inhibitor with IC50s of 6 nM, 4 nM, 15 nM and 1 nM, respectively.

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

Telatinib mesylate Chemical Structure

Telatinib mesylate Chemical Structure

CAS No. : 332013-26-0

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Based on 1 publication(s) in Google Scholar

Other Forms of Telatinib mesylate:

Telatinib mesylate Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Telatinib mesylate

View All VEGFR Isoform Specific Products:

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

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PDGFR PDGFRβ PDGFRα

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Telatinib mesylate (Bay 57-9352 mesylate) is a potent and orally active VEGFR2, VEGFR3, PDGFα, and c-Kit inhibitor with IC50s of 6 nM, 4 nM, 15 nM and 1 nM, respectively[1].

IC50 & Target[1]

VEGFR2

6 nM (IC50)

VEGFR3

4 nM (IC50)

PDGFRα

15 nM (IC50)

c-Kit

1 nM (IC50)

In Vitro

Telatinib enhances the anticancer activity of ABCG2 substrate anticancer drugs by inhibiting ATP-binding cassette G2 (ABCG2) efflux transporter activity. Co-incubation of ABCG2-overexpressing drug resistant cell lines with Telatinib and ABCG2 substrate anticancer drugs significantly reduces cellular viability, whereas Telatinib alone does not significantly affect drug sensitive and drug resistant cell lines. Telatinib at 1 μM does not significantly alter the expression of ABCG2 in ABCG2-overexpressing cell lines. Telatinib at 1 μM significantly enhances the intracellular accumulation of [3H]-mitoxantrone (MX) in ABCG2-overexpressing cell lines[2].
Telatinib at 1 μM significantly reduces the rate of [3H]-MX efflux from ABCG2-overexpressing cells. Furthermore, Telatinib significantly inhibits ABCG2-mediated transport of [3H]-E₂17βG in ABCG2 overexpressing membrane vesicles[2].

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

Telatinib mesylate Related Antibodies
In Vivo

Telatinib (15 mg/kg; oral dministration; every 2nd and 3rd day; total 12 times; male athymic NCR (nu/nu) nude mice) with Doxorubicin (1.8 mg/kg) significantly decreases the growth rate and tumor size of ABCG2 overexpressing tumors in a xenograft nude mouse model[2].

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

Animal Model: Male athymic NCR (nu/nu) nude mice (13-15 g, age 4-5 weeks) injected with H460 and H460/MX20 cells[2]
Dosage: 15 mg/kg
Administration: Oral dministration; every 2nd and 3rd day; total 12 times
Result: With Doxorubicin (1.8 mg/kg) significantly decreased the growth rate and tumor size of ABCG2 overexpressing tumors in a xenograft nude mouse model.
Clinical Trial
Molecular Weight

505.93

Formula

C21H20ClN5O6S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=NC=CC(COC2=NN=C(NC3=CC=C(Cl)C=C3)C4=C2OC=C4)=C1)NC.OS(=O)(C)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°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: 

DMSO : 250 mg/mL (494.14 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9766 mL 9.8828 mL 19.7656 mL
5 mM 0.3953 mL 1.9766 mL 3.9531 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
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
DMSO 1 mM 1.9766 mL 9.8828 mL 19.7656 mL 49.4140 mL
5 mM 0.3953 mL 1.9766 mL 3.9531 mL 9.8828 mL
10 mM 0.1977 mL 0.9883 mL 1.9766 mL 4.9414 mL
15 mM 0.1318 mL 0.6589 mL 1.3177 mL 3.2943 mL
20 mM 0.0988 mL 0.4941 mL 0.9883 mL 2.4707 mL
25 mM 0.0791 mL 0.3953 mL 0.7906 mL 1.9766 mL
30 mM 0.0659 mL 0.3294 mL 0.6589 mL 1.6471 mL
40 mM 0.0494 mL 0.2471 mL 0.4941 mL 1.2353 mL
50 mM 0.0395 mL 0.1977 mL 0.3953 mL 0.9883 mL
60 mM 0.0329 mL 0.1647 mL 0.3294 mL 0.8236 mL
80 mM 0.0247 mL 0.1235 mL 0.2471 mL 0.6177 mL
100 mM 0.0198 mL 0.0988 mL 0.1977 mL 0.4941 mL
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Telatinib mesylate 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:

Telatinib332013-26-0Bay 57-9352VEGFRPDGFRc-KitVascular endothelial growth factor receptorPlatelet-derived growth factor receptorSCFRCD117VEGFR2VEGFR3PDGFαangiogenesisorallyvascularhypertensionABCG2Inhibitorinhibitorinhibit

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