Pazopanib Hydrochloride

Pazopanib Hydrochloride 구조식 이미지
카스 번호:
635702-64-6
상품명:
Pazopanib Hydrochloride
동의어(영문):
Pazopanib hydrochloride;Pazopanib HCl;ArMala;786034;CS-462;GW-786034B;GW786034 HCl;Votrient HCl;Pazopanib HCI;Unii-33Y9anm545
CBNumber:
CB42495435
분자식:
C21H24ClN7O2S
포뮬러 무게:
473.98
MOL 파일:
635702-64-6.mol

Pazopanib Hydrochloride 속성

녹는점
>290°C (dec.)
저장 조건
Hygroscopic, Refrigerator, under inert atmosphere
용해도
아세토니트릴(약간), DMSO(약간)에 용해됨
물리적 상태
노란색 가루.
색상
흰색에서 황백색까지
안정성
흡습성
안전
  • 위험 및 안전 성명
  • 위험 및 사전주의 사항 (GHS)
그림문자(GHS): GHS hazard pictograms
신호 어: Warning
유해·위험 문구:
암호 유해·위험 문구 위험 등급 범주 신호 어 그림 문자 P- 코드
H302 삼키면 유해함 급성 독성 물질 - 경구 구분 4 경고 GHS hazard pictograms P264, P270, P301+P312, P330, P501
H315 피부에 자극을 일으킴 피부부식성 또는 자극성물질 구분 2 경고 GHS hazard pictograms P264, P280, P302+P352, P321,P332+P313, P362
H319 눈에 심한 자극을 일으킴 심한 눈 손상 또는 자극성 물질 구분 2A 경고 GHS hazard pictograms P264, P280, P305+P351+P338,P337+P313P
H332 흡입하면 유해함 급성 독성 물질 흡입 구분 4 경고 GHS hazard pictograms P261, P271, P304+P340, P312
H335 호흡 자극성을 일으킬 수 있음 특정 표적장기 독성 - 1회 노출;호흡기계 자극 구분 3 경고 GHS hazard pictograms
예방조치문구:
P261 분진·흄·가스·미스트·증기·...·스프레이의 흡입을 피하시오.
P280 보호장갑/보호의/보안경/안면보호구를 착용하시오.
P305+P351+P338 눈에 묻으면 몇 분간 물로 조심해서 씻으시오. 가능하면 콘택트렌즈를 제거하시오. 계속 씻으시오.

Pazopanib Hydrochloride C화학적 특성, 용도, 생산

개요

Pazopanib Hydrochloride is the hydrochloride salt of a small molecule inhibitor of multiple protein tyrosine kinases with potential antineoplastic activity. It is an oral second-generation multitarget TKI developed by GSK and approved for marketing by the FDA in 2009 and the EMA in 2010. It targets the VEGFR, platelet-derived growth factor receptor, and c-kit, key proteins responsible for tumor growth and survival. It is used to treat patients with advanced RCC and advanced soft tissue sarcoma who have experienced chemotherapy. Pazopanib Hydrochloride has a role as an antineoplastic agent, a vascular endothelial growth factor receptor antagonist, a tyrosine kinase inhibitor, and an angiogenesis-modulating agent.

용도

Pazopanib Hydrochloride (GW786034, Votrient, Armala) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM, respectively.

정의

ChEBI: A hydrochloride salt prepared from equimolar amounts of pazopanib and hydrochloric acid. Used for treatment of kidney cancer.

Clinical Use

Pazopanib is a potent and selective multi-targeted receptor tyrosine kinase inhibitor of VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-a/b, and c-kit that blocks tumor growth and inhibits angiogenesis. It was approved for renal cell carcinoma by the U.S. Food and Drug Administration in 2009 and is marketed under the trade name Votrient by the drug’s manufacturer, GlaxoSmithKline.

부작용

Pazopanib is synthesized in five chemical steps starting from 3-methyl-6-nitroindazole, which is converted to the corresponding 2,3-dimethylindazole analog via N-methylation with trimethyloxonium tetrafluoroborate. Subsequent reduction of the nitro group to the amino group using tin chloride followed by condensation with 2,4dichloropyrimidine yields a chloropyrimidinylaminoindazole intermediate. The final two steps leading up to pazopanib consist of an N-methylation reaction using iodomethane and cesium carbonate followed by condensation with 5-amino-2-methylbenzenesulfonamide.

참고 문헌

[1] Sodeifian, G. et al. “Solubility of pazopanib hydrochloride (PZH, anticancer drug) in supercritical CO2: Experimental and thermodynamic modeling.” The Journal of Supercritical Fluids 55 1 (2022): 0.
[2] “Stability Indicating HPTLC Method Development and Validation for the Estimation of Pazopanib Hydrochloride in Bulk and its Dosage Form.” International Journal of Pharmaceutical Research 18 1 (2020).
[3] K. Kawasaki . “Retrospective Safety Analysis in Advanced Soft Tissue Sarcoma Patients of Pazopanib Hydrochloride.” Annals of Oncology 24 (2013): Page ix38.
[4] Gupta, Amit and Rashmi Dahima. “Application of Simplex Lattice Mixture design and desirability function in the development and Optimization of SEDDS for protein kinase inhibitor-Pazopanib Hydrochloride.” Research Journal of Pharmacy and Technology 83 1 (2023): 0.

Pazopanib Hydrochloride 준비 용품 및 원자재

원자재

준비 용품


Pazopanib Hydrochloride 공급 업체

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