332012-40-5 Usage
Description
Telatinib, also known as BAY 57-9352, is an orally available, potent multitargeted inhibitor of VEGFR-2, VEGFR-3, PDGFR-β, and c-Kit tyrosine kinases. It exhibits high potency with IC50 values of 19 nM, 6 nM, 4 nM, 15 nM, and 1 nM for VEGFR-2 autophosphorylation, VEGFR3, PDGFRα, and c-Kit, respectively. Additionally, Telatinib binds to the transmembrane region of the ABCG2 efflux transporter, enhancing the intracellular accumulation of certain drugs in ABCG2-overexpressing cells. It has demonstrated the ability to decrease tumor growth rate and size in specific mouse xenograft models.
Uses
Used in Oncology:
Telatinib is used therapeutically as a small-molecule inhibitor targeting vascular endothelial growth factor receptors 2 and 3 (VEGFR-2/-3) and platelet-derived growth factor receptor β (PDGFR-β) tyrosine kinases. It is particularly beneficial for patients with advanced solid tumors, as it helps in inhibiting the growth and progression of these tumors by targeting the specific kinases involved in tumor angiogenesis and growth.
Used in Drug Resistance Modulation:
Telatinib also has the potential to be used in overcoming drug resistance in cancer treatment. By binding to the ABCG2 efflux transporter, it can enhance the intracellular accumulation of certain drugs, making it a valuable tool in combination therapies to improve the efficacy of existing chemotherapeutic agents, especially in cases where tumors have developed resistance to standard treatments.
references
[1]. steeghs, n., et al., hypertension and rarefaction during treatment with telatinib, a small molecule angiogenesis inhibitor. clin cancer res, 2008. 14(11): p. 3470-6.[2]. strumberg, d., et al., phase i dose escalation study of telatinib (bay 57-9352) in patients with advanced solid tumours. br j cancer, 2008. 99(10): p. 1579-85.[3]. sodani, k., et al., telatinib reverses chemotherapeutic multidrug resistance mediated by abcg2 efflux transporter in vitro and in vivo. biochem pharmacol, 2014. 89(1): p. 52-61. [4]. eskens, f.a., et al., phase i dose escalation study of telatinib, a tyrosine kinase inhibitor of vascular endothelial growth factor receptor 2 and 3, platelet-derived growth factor receptor beta, and c-kit, in patients with advanced or metastatic solid tumors. j clin oncol, 2009. 27(25): p. 4169-76.
Check Digit Verification of cas no
The CAS Registry Mumber 332012-40-5 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 3,3,2,0,1 and 2 respectively; the second part has 2 digits, 4 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 332012-40:
(8*3)+(7*3)+(6*2)+(5*0)+(4*1)+(3*2)+(2*4)+(1*0)=75
75 % 10 = 5
So 332012-40-5 is a valid CAS Registry Number.
332012-40-5Relevant articles and documents
Industrial production method tela for Nepal of methanesulfonic acid
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, (2017/02/02)
The invention provides an industrial production method of telatinib mesylate. According to the method, 2-methylamino carbonyl-4-picolinic acid ethyl ester is used as a raw material, sodium borohydride is used as a reducing agent, or sodium borohydride and Lewis acid are selected for catalytic reduction, 2-methylamino carbonyl-4-pyridinemethanol is obtained after reduction in an organic solvent, an intermediate 2-methylamino carbonyl-4-pyridinemethanol hydrochloride monohydrate is obtained through salt formation, the 2-methylamino carbonyl-4-pyridinemethanol hydrochloride monohydrate and 4-chloro-anilino-7-chlorofuro[2,3-d]pyridazine have a condensation reaction under the action of potassium tert-butoxide to form telatinib free alkali, the telatinib free alkali reacts with methane sulfonic acid to form salt finally, and the telatinib mesylate is obtained through cooling and crystallization. The process operation is simple and safe, reaction conditions are mild, the obtained product is high in purity and meets the quality requirement, and the method is suitable for large-scale industrial production.
COMPOUNDS FOR TREATING PULMONARY HYPERTENSION
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, (2008/06/13)
The present invention relates to pharmaceutical compositions and combinations for treating, preventing or managing pulmonary hypertension comprising small molecule heterocyclic pharmaceuticals, and more particularly, substituted pyridines and pyridazines optionally combined with at least one additional therapeutic agent.
