化学信息：
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化学名
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N-[4-(3-bromoanilino)quinazolin-6-yl]but-2-ynamide
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简称
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CL-387785
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别名
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EKI-785, WAY-EKI 785, CL387785, CL 387785, EKI785, WAY-EKI785, EKI 785
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中文名
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N/A
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化学式
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C18H13BrN4O
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分子量
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381.23
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CAS号
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194423-06-8
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纯度
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98%
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溶剂/溶解度
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Water<1mg/ml; DMSO14mg/ml; Ethanol<1mg/ml
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溶液配制
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5mg加入1.31ml DMSO，或者每3.81mg加入1ml DMSO，配制成10mM溶液。SD4785-10mM用DMSO配制。
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生物信息：
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产品描述
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CL-387785 (EKI785; WAY-EKI 785) is an irreversible inhibitor of EGFR with IC50 of 370+/-120pM; is able to overcome resistance caused by the T790M mutation on a functional level.
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信号通路
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JAK/STAT; Protein Tyrosine Kinase
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靶点
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EGFR
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－
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－
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－
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－
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IC50
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370+/-120 pM
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－
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－
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－
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－
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体外研究
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CL-387785 blocked EGF-stimulated autophosphorylation of the receptor in cells (IC50 approximately 5nM), inhibited cell proliferation (IC50=31-125nM) primarily in a cytostatic manner in cell lines that overexpress EGF-R or c-erbB-2. Whereas transformation by most EGFR mutants confers on cells sensitivity to erlotinib and gefitinib, transformation by an exon 20 insertion makes cells resistant to these inhibitors but more sensitive to the irreversible inhibitor CL-387,785. CL-387,785 is able to overcome resistance caused by the T790M mutation on a functional level, correlating with effective inhibition of downstream signaling pathways.
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体内研究
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CL-387785 profoundly blocked the growth of a tumor that overexpresses EGF-R in nude mice (when given orally at 80mg/kg/day for 10 days, daily). Treatment of BPK mice with EKI-785 resulted in a marked reduction of collecting tubule (CT) cystic lesions, improved renal function, decreased biliary epithelial abnormalities, and an increased life span. Cystic animals treated with EKI-785 to postnatal day 48 (P-48) were alive and well with normal renal function, a reduced CT cystic index of 2.0 (P<0.02), a threefold increased in maximum urinary concentrating ability (P<0.01), and a significant decrease in biliary epithelial proliferation/fibrosis (P<0.01).
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临床实验
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N/A
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特征
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N/A
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相关实验数据(此数据来自于公开文献，碧云天并不保证其有效性)：
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酶活性检测实验
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方法
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N/A
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细胞实验
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细胞系
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N/A
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浓度
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N/A
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处理时间
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N/A
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方法
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N/A
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动物实验
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动物模型
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N/A
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配制
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N/A
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剂量
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N/A
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给药方式
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N/A
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参考文献：
1. Discafani CM, et al. Biochem Pharmacol. 1999 Apr 15, 57(8), 917-25.
2. Sweeney WE, et al. Kidney Int. 2000 Jan, 57(1), 33-40.
3. Greulich H, et al. PLoS Med. 2005 Nov, 2(11), e313.
4. Kobayashi S, et al. Cancer Res. 2005 Aug 15, 65(16), 7096-101.
包装清单：
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产品编号
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产品名称
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包装
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SD4785-10mM
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CL-387785 (EGFR抑制剂)
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10mM×0.2ml
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SD4785-5mg
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CL-387785 (EGFR抑制剂)
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5mg
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SD4785-25mg
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CL-387785 (EGFR抑制剂)
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25mg
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—
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说明书
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1份
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保存条件：
-20℃保存，至少一年有效。5mg和25mg包装也可室温保存，至少6个月有效。如果溶于非DMSO溶剂，建议分装后-80℃保存，预计6个月内有效。
注意事项：
本产品对人体有害，操作时请小心，并注意有效防护以避免直接接触人体或吸入体内。
本产品仅限于专业人员的科学研究用，不得用于临床诊断或治疗，不得用于食品或药品，不得存放于普通住宅内。
为了您的安全和健康，请穿实验服并戴一次性手套操作。
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