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

Telatinib mesylate (Synonyms: Bay 57-9352 mesylate)

Cat. No.: HY-10527C Purity: 99.46%
Handling Instructions

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

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1 Publications Citing Use of MCE Telatinib mesylate

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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].

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

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].

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.
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)

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
10 mM 0.1977 mL 0.9883 mL 1.9766 mL
*Please refer to the solubility information to select the appropriate solvent.
Purity & Documentation
References
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Product Name:
Telatinib mesylate
Cat. No.:
HY-10527C
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