產(chǎn)品目錄

規(guī)格	10mg 50mg
CAS	859853-30-8
別名	BMS690514;BMS 690514
化學名	(3R,4R)-4-amino-1-[[4-(3-methoxyanilino)pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]piperidin-3-ol
分子式	C19H24N6O2
分子量	368.44
溶解度	Soluble in DMSO
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

BMS-690514, a potent inhibitor of human epidermal growth factor receptor (HER/EGFR). In addition to an improved potency in inhibiting HER1/HER2 with IC50 value of 5 and 19 nM, respectively, BMS-690514 also shows significant potency against other protein kinases, such as VEGFR2, Flt-3, and Lck with IC50 value of 50, 110, and 220 nM, respectively.[1]

The epidermal growth factor receptor is a member of the ErbB family of receptors, EGFR (ErbB-1), HER2/c-neu (ErbB-2), Her 3 (ErbB-3) and Her 4 (ErbB-4) [2]. Upon activation by its growth factor ligands, EGFR undergoes a transition from an inactive monomeric form to an active homodimer[3]. In addition to forming homodimers after ligand binding, EGFR may pair with another member of the ErbB receptor family, such as ErbB2/Her2/neu, to create an activated heterodimer. EGFR dimerization stimulates its intrinsic intracellular protein-tyrosine kinase activity, resulting autophosphorylation[4], which elicits downstream activation and signaling by several other proteins with SH2 domains that can initiate several signal transduction cascades, principally the MAPK, Akt and JNK pathways, leading to DNA synthesis and cell proliferation.[5]

Mutations affecting EGFR expression or activity could result in cancer.[6] BMS-690514 is an oral oncologic agent being developed for the treatment of patients with advanced nonsmall cell lung cancer and other solid tumor, for inhibiting the EGFR tyrosine kinase, which is on the cytoplasmic side of the receptor. Without kinase activity, EGFR is unable to activate itself, which is a prerequisite for binding of downstream adaptor proteins. Ostensibly by halting the signaling cascade in cells that rely on this pathway for growth, tumor proliferation and migration is diminished. BMS-690514 is metabolized via multiple metabolic pathways, including P450-mediated oxidation at one of the carbons of its pyrrolotriazine group at this site results in the formation of two metabolites, M1 and M37, through HPLC, NMR, LC/MS/MS and radiochromatographic analysis[7

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1. 本產(chǎn)品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區(qū)。

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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