Telatinib mesylate

Modify Date: 2024-01-08 04:13:11

Telatinib mesylate structure	Common Name	Telatinib mesylate
	CAS Number	332013-26-0	Molecular Weight	505.93
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₂₁H₂₀ClN₅O₆S	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of Telatinib mesylate

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].

Name	Telatinib mesylate

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].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Protein Tyrosine Kinase/RTK >> PDGFR Signaling Pathways >> Protein Tyrosine Kinase/RTK >> VEGFR Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Kit
Target	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].
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]. 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.
References	[1]. Steeghs N, et al.Hypertension and rarefaction during treatment with telatinib, a small molecule angiogenesis inhibitor.Clin Cancer Res. 2008 Jun 1;14(11):3470-6. [2]. [2] Sodani K, et al. Telatinib reverses chemotherapeutic multidrug resistance mediated by ABCG2 efflux transporter in vitro and in vivo. Biochem Pharmacol. 2014 May 1;89(1):52-61.

Molecular Formula	C₂₁H₂₀ClN₅O₆S
Molecular Weight	505.93

DC Chemicals Limited
China
Product Name: Telatinib mesylate
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Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

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