DC Chemicals Limited
China
Product Name: Telatinib
Price: $550.0/100mg $1000.0/250mg $1900.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

332012-40-5

332012-40-5 structure

Name: Telatinib
Chemical Name: 4-[[4-(4-chloroanilino)furo[2,3-d]pyridazin-7-yl]oxymethyl]-N-methylpyridine-2-carboxamide
CAS Number: 332012-40-5
Molecular Formula: C₂₀H₁₆ClN₅O₃
Molecular Weight: 409.826
Catalog: API Antineoplastic agents Tinic antineoplastic agents
Create Date: 2018-08-05 12:12:23
Modify Date: 2024-01-02 23:30:04
Telatinib (Bay 57-9352) is an orally active, small molecule inhibitor of VEGFR2, VEGFR3, PDGFα, and c-Kit with IC50s of 6, 4, 15 and 1 nM, respectively.

Name	4-[[4-(4-chloroanilino)furo[2,3-d]pyridazin-7-yl]oxymethyl]-N-methylpyridine-2-carboxamide
Synonyms	Telatinib,BAY 57-9352,BAY 57-9352 4-(4-(4-chloro-phenylamino)-furo[2,3-d]pyridazin-7-yloxymethyl)-pyridine-2-carboxylic acid methylamide S2231_Selleck BAY57-9352 Telatinib 4-[({4-[(4-Chlorophenyl)amino]furo[2,3-d]pyridazin-7-yl}oxy)methyl]-N-methyl-2-pyridinecarboxamide Bay 57-9352 UNII:18P7197Q7J 4-(4-chlorophenylamino)-7-(2-methylaminocarbonyl-4-pyridylmethoxy)furo-[2,3-d]pyridazine 4-((4-(4-chlorophenylamino)furo[2,3-d]pyridazin-7-yloxy)methyl)-N-methylpicolinamide 2-Pyridinecarboxamide, 4-[[[4-[(4-chlorophenyl)amino]furo[2,3-d]pyridazin-7-yl]oxy]methyl]-N-methyl- BAY-579352

Description	Telatinib (Bay 57-9352) is an orally active, small molecule inhibitor of VEGFR2, VEGFR3, PDGFα, and c-Kit with IC50s of 6, 4, 15 and 1 nM, respectively.
Related Catalog	Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Kit Research Areas >> Cancer
Target	VEGFR2:6 nM (IC50) VEGFR3:4 nM (IC50) PDGFRα:15 nM (IC50) c-Kit:1 nM (IC50)
In Vitro	Telatinib has low affinity for the Raf kinase pathway, epidermal growth factor receptor family, the fibroblast growth factor receptor (FGFR) family, or the Tie-2 receptor[2]. Telatinib is metabolized by various cytochrome P450 (CYP) isoforms including CYP3A4/3A5, CYP2C8, CYP2C9, and CYP2C19 as well as by uridine diphosphate glucuronosyltransferase 1A4 (UGT1A4), with the formation of the N-glucuronides of telatinib as the major biotransformation pathway in man. In vitro studies show telatinib to be a weak substrate of the adenosine triphosphate binding cassette (ABC) B1 (ABCB1) transporter[3]. Telatinib at 1 μM significantly enhances the intracellular accumulation of [3H]-mitoxantrone (MX) in ABCG2-overexpressing cell lines. In addition, 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[4].
In Vivo	Telatinib causes a significant decrease in endothelium-dependent and endothelium-independent vasodilation. VEGF inhibition by itself decreases NO synthesis, which promotes vasoconstriction, increases peripheral resistance, and therefore can induce an increase in blood pressure[1]. Telatinib (15 mg/kg) with doxorubicin (1.8 mg/kg) significantly decreases the growth rate and tumor size of ABCG2 overexpressing tumors in a xenograft nude mouse model[4].
Kinase Assay	The vanadate (Vi)-sensitive ATPase activity of ABCG2 in the membrane of High Five insect cells is measured. Briefly, membrane (2 μg/0.06 mL) are incubated in ATPase assay buffer with or without 0.4 mM vanadate at 37°C for 5 min and then incubated with varying concentrations of telatinib at 37°C for 5 min. The ATPase reaction is started by the addition of 4 mM Mg-ATP. After incubating at 37°C for 10 min, the reactions are stopped by adding 0.05 mL of 10% SDS solution. The liberated inorganic phosphate is measured[4].
Animal Admin	Mice: The mice are randomized into four groups and treated with one of the following regimens: (a) vehicle (10% N-methyl-pyrrolidinone, 90% polyethylene glycol 300) (q3d×6), (b) DOX (1.8 mg/kg, i.p., q3d×6), (c) telatinib dissolved in 10% N-methyl-pyrrolidinone, 90% polyethylene glycol 300 (15 mg/kg, p.o., every 2nd and 3rd day; total 12 times), and (d) DOX (1.8 mg/kg, i.p., q3d×6) + telatinib (15 mg/kg, p.o., every 2nd and 3rd day, given 1 h before giving DOX; total 12 times). DOX for injection is prepared by dissolving in saline. Tumor volume is measured using calipers and body weights are recorded[4].
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]. Langenberg MH, et al. Phase I evaluation of telatinib, a vascular endothelial growth factor receptor tyrosine kinase inhibitor, in combination with irinotecan and capecitabine in patients with advanced solid tumors. Clin Cancer Res. 2010 Apr 1;16(7):2187-97. [3]. Steeghs N, et al. Pharmacogenetics of telatinib, a VEGFR-2 and VEGFR-3 tyrosine kinase inhibitor, used in patients with solid tumors. Invest New Drugs. 2011 Feb;29(1):137-43. [4]. 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.

Density	1.4±0.1 g/cm3
Boiling Point	713.6±60.0 °C at 760 mmHg
Molecular Formula	C₂₀H₁₆ClN₅O₃
Molecular Weight	409.826
Flash Point	385.4±32.9 °C
Exact Mass	409.094177
PSA	102.17000
LogP	2.53
Vapour Pressure	0.0±2.3 mmHg at 25°C
Index of Refraction	1.684
Storage condition	-20℃

332013-43-1

332013-41-9

~45%

332012-40-5

Literature: BAYER CORPORATION Patent: EP1228063 B1, 2009 ; Location in patent: Page/Page column 45-46 ;

332013-43-1

332013-40-8

~46%

332012-40-5

Literature: Bayer Pharmaceuticals Corporation Patent: US6689883 B1, 2004 ; Location in patent: Page column 61 ;

Precursor 3
332013-43-1 332013-41-9 332013-40-8
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