產(chǎn)品目錄

規(guī)格	250mg 500mg
CAS	1257628-64-0
別名	N/A
化學(xué)名	N/A
分子式	C29H27F3N6O
分子量	532.56
溶解度	Soluble in DMSO
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：

GZD856 is a novel and orally bioavailable PDGFRα/β inhibitor with IC50s of 68.6 and 136.6 nM, respectively. Anti-lung cancer activities[1]. Also a Bcr-AblT315I inhibitor with IC50s of 19.9 and 15.4 nM for Bcr-Abl and T315I mutant[2].

GZD856 (0.0032-10 μM) exerts antiproliferative activity against a panel of lung cancer cells[1].GZD856 shows dose-dependent inhibition of PDGFRα and PDGFRβ phosphorylation in H1703 and A549 cells, respectively. The activation of downstream AKT (phosphorylation of S473 but not T308), ERK1/2 and STAT3 is also observed after exposure to GZD856, with no obvious effects on total protein levels[1].GZD856 induces dose-dependent G0/G1 phase arrest and apoptosis in H1703 cells but not in A549 cells[1].GZD856 strongly suppresses the proliferation of K562, K562R (Q252H) and murine Ba/F3 cells ectopically expressing Bcr-AblWT and Bcr-AblT315I, with IC50s of 2.2, 67.0, 0.64 and 10.8 nM, respectively[2].

GZD856 (10 and 30 mg/kg/day) displays good in vivo antitumor activity in both H1703 and A549 lung cancer models[1]. GZD856 exhibits dose-dependent suppression of PDGFRα and PDGFRβ activation and downstream signaling in H1703 and A549 tumor tissues[1]. GZD856 displays promising in vivo therapeutic effects on PDGFRα-/PDGFRβ+ A549 cancer cells in a Luc orthotopic model, inhibiting both tumor growth and tumor metastasis[1].GZD856 potently suppresses tumor growth in mouse bearing xenograft K562 and Ba/F3 cells expressing Bcr-AblT315I[2].

[1]. Zhang Z, et al. GZD856, a novel potent PDGFRα/β inhibitor, suppresses the growth and migration of lung cancer cells in vitro and in vivo. Cancer Lett. 2016 May 28;375(1):172-178. [2]. Lu X, et al. Synthesis and identification of GZD856 as an orally bioavailable Bcr-AblT315I inhibitor overcoming acquired imatinib resistance. J Enzyme Inhib Med Chem. 2017 Dec;32(1):331-336.

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)。

2. 為了您的安全和健康，請(qǐng)穿好實(shí)驗(yàn)服并佩戴一次性手套和口罩操作。

原創(chuàng)作者：上海莼試生物技術(shù)有限公司

在線咨詢

留言注意事項(xiàng)：

1.遵守中華人民共和國(guó)有關(guān)法律、法規(guī)，尊重網(wǎng)上道德，承擔(dān)一切因您的行為而直接或間接引起的法律責(zé)任。

2.請(qǐng)您真實(shí)的反映產(chǎn)品的情況,不要捏造、誣蔑、造謠。如對(duì)產(chǎn)品有任何疑問(wèn),也可以留言咨詢。

3.未經(jīng)本站同意，任何人不得利用本留言簿發(fā)布個(gè)人或團(tuán)體的具有廣告性質(zhì)的信息或類似言論。

您感興趣的產(chǎn)品*
您的單位*
聯(lián)系人*
聯(lián)系電話*
詳細(xì)地址*
常用郵箱*
請(qǐng)輸入您對(duì)我們的意見(jiàn)或建議*
驗(yàn)證碼*