| Identification | Back Directory | [Name]
Telatinib mesylate | [CAS]
332013-26-0 | [Synonyms]
Telatinib mesylate
Telatinib mesylate (Bay 57-9352 mesylate)
4-(((4-((4-chlorophenyl)amino)furo[2,3-d]pyridazin-7-yl)oxy)methyl)-N-methylpicolinamide methanesulfonate | [Molecular Formula]
C21H20ClN5O6S | [MOL File]
332013-26-0.mol | [Molecular Weight]
505.93 |
| Hazard Information | Back Directory | [Uses]
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]. | [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. |
| [IC 50]
VEGFR2: 6 nM (IC50); VEGFR3: 4 nM (IC50); PDGFRα: 15 nM (IC50); c-Kit: 1 nM (IC50) | [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. DOI:10.1158/1078-0432.CCR-07-5050
[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. DOI:10.1016/j.bcp.2014.02.012 |
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| Company Name: |
InvivoChem
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| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
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