產(chǎn)品目錄

規(guī)格	5mg 25mg 100mg
CAS	915769-50-5
別名
化學(xué)名	4-amino-5-fluoro-3-(6-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazol-2-yl)quinolin-2(1H)-one 2-hydroxypropanoate hydra
分子式	C24H29FN6O5
分子量	500.52
溶解度	≥ 168.2mg/mL in H2O
儲(chǔ)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：

Description:

IC50: ~10 nmol/L for FGFR1–3

Fibroblast growth factor receptor 1 (FGFR1) and FGFR2 amplifications are observed in approximately 10% of breast cancers and are related to poor outcomes. Dovitinib (TKI258) is an oral tyrosine kinase inhibitor (TKI) against FGFR1–3, VEGFR1–3, and platelet-derived growth factor receptor (PDGFR).

In vitro: Dovitinib decreased the concentrations of pFRS2 and pERK/MAPK in a dose-dependent manner in FGFR1 amplified and FGFR2 amplified cell lines. The IC50 for cell growth inhibition was 190 and 180 nmol/L in MDA-MB-134 and SUM52, respectively. Conversely, IC50 values were more than 2,000 nmol/L in the 11 breast cancer cell lines that had neither FGFR1 nor FGFR2 amplification [1].

In vivo: In vivo model (HBCx-2 breast cancer primary xenograft, with 8 FGFR1 gene copies), dovitinib prevented tumor growth at the 30 mg/kg dose and caused tumor regression at the 50 mg/kg dose. Similarly, dovitinib caused tumor regression in HBCx-3 xenografts when administered at a dose of 40 mg/kg daily until day 35 [1].

Clinical trial: Eighty-one patients were enrolled in the trial. Unconfirmed response or stable disease for over 6 months was observed in 5 and 1 patient(s) with FGFR1-amplified/HR-positive and FGFR1-nonamplified/HR-positive breast cancer. When qPCR-identified amplifications in FGFR1, FGFR2, or FGF3 were grouped to define an FGF pathway–amplified breast cancer in HR-positive patients, the mean reduction in target lesions was 21.1% compared with a 12.0% increase in patients that did not present with FGF pathway–amplified breast cancer [1].

特別提醒：

1. 本產(chǎn)品僅供科研使用。請(qǐng)勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請(qǐng)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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