PD 166285

PD 166285 C화학적 특성, 용도, 생산

화학적 성질

Yellow Solid

용도

A broad-spectrum receptor tyrosine kinase (RTK) inhibitor which shows anti-angiogenic activity and anti-tumor efficacy in combination with photodynamic therapy (PDT).

일반 설명

A cell-permeable, orally bioavailable, ATP-competitive, broad-spectrum tyrosine kinase inhibitor (IC₅₀ against against c-Src, Wee1, FGFR-1, Myt1, EGFR, and PDGFRβ = 8.4, 24, 39.3, 72, 87.5 and 98.3 nM, respectively) that suppresses angiogenesis both in vitro (max inhibition dose at 100 nM in HUVEC microcapillary formation assays) and in vivo (max inhibition achieved via 5 mg/kg p.o. in murine Matrigel plug angiogenesis assays), while exhibiting much reduced potency against Chk1, MAPK, and PKC (IC₅₀ = 3.4, 5, and 22.7 μM, respectively) and little activity toward IRTK and Cdk4/D1 even at concentrations as high as 50 μM. Shown to effectively block PDGF-, EGF-, and bFGF-stimulated receptor phosphorylations (IC₅₀ = 6.5, 1600, and 97.3 nM, respectively) and other cellular responses in rat aortic smooth muscle cells. Inhibition of cellular Wee1 activity by 500 nM PD 166285 in combination with 50 ng/ml nocodazole (Cat. No. 487928) treatment is also reported to result in a blockage of radiation-induced Cdc2 phosphorylation on Tyr15 and Thr14 in 7 human cancer cells and specifically demonstrated to sensatize PA-1 cultures to radiation-induced cell death in a p53-dependent manner.

생물학적 활성

Potent inhibitor of the tyrosine kinases c-Src, fibroblast growth factor receptor 1 (FGFR1), and platelet-derived growth factor receptor β (PDGFR β ) (IC 50 values are 8.4, 39.3 and 98.3 nM respectively). Also inhibits the checkpoint kinases Wee1 and Myt1; abolishes Cdc2 phosphorylation in numerous tumor cell lines and abrogates the G 2 checkpoint.

PD 166285 준비 용품 및 원자재

원자재

준비 용품

PD 166285 공급 업체

공급자	전화	이메일	국가	제품 수	이점
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32760	60
career henan chemical co	+86-0371-86658258 +8613203830695	factory@coreychem.com	China	29825	58
Shaanxi Dideu Medichem Co. Ltd	+86-029-89586680 +86-18192503167	1026@dideu.com	China	8853	58
Hefei Hirisun Pharmatech Co., Ltd	+8615056975894	shawn@hirisunpharm.com	CHINA	9923	58
LEAP CHEM CO., LTD.	+86-852-30606658	market18@leapchem.com	China	24738	58
Nantong HI-FUTURE Biology Co., Ltd.	+undefined18051384581	sales@chemhifuture.com	China	3136	58
TargetMol Chemicals Inc.	+1-781-999-5354	support@targetmol.com	United States	19973	58
Wuhan Topule Biopharmaceutical Co., Ltd	+8618327326525	masar@topule.com	China	8474	58
Shenyang Zhongshen Zekang Biomedical Technology Research Co., Ltd	+86-18341751992 +86-15382112998	757984502@qq.com	China	892	58
Hangzhou ChangCun Biotechnology Co., Ltd.	0571-; 13567100326	158848739@qq.com	China	108	50

PD 166285 관련 검색: