您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > JBJ-09-063
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
JBJ-09-063
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
JBJ-09-063图片
CAS NO:2820336-67-0
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
JBJ-09-063 是一种突变选择性变构EGFR抑制剂,对 EGFR L858R、EGFR L858R/T790M、EGFR L858R/T790M/C797S 和 EGFRLT/L747S 的IC50分别为 0.147 nM、0.063 nM、0.083 nM 和 0.396 nM。JBJ-09-063 有效降低 EGFR、Akt 和 ERK1/2 磷酸化。JBJ-09-063 对 EGFR 酪氨酸激酶抑制剂 (TKI) 敏感与耐药模型均有效。JBJ-09-063 可用于 EGFR 突变型肺癌研究。
生物活性

JBJ-09-063 is a mutant-selective allostericEGFRinhibitor withIC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM forEGFRL858R,EGFRL858R/T790M,EGFRL858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 effectively reducesEGFR,Aktand ERK1/2 phosphorylation. JBJ-09-063 is effective acrossEGFRtyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 can be used for researching EGFR-mutant lungcancer[1].

IC50& Target[1]

EGFR L858R

0.147 nM (IC50)

EGFR L858R/T790M

0.063 nM (IC50)

EGFR L858R/T790M/C797S

0.083 nM (IC50)

EGFRLT/L747S

0.396 nM (IC50)

体外研究
(In Vitro)

JBJ-09-063 is remarkably effective at inhibiting cell growth and leads to a significant increase in apoptosis, even though H3255GR cells are resistant to gefitinib as a single agent, as they contain an EGFR T790M mutation[1].
JBJ-09-063 is effective in H1975 cells exogenously expressing the osimertinib-resistant mutations[1].
JBJ-09-063 exhibits IC50s of 50 nM and 6 nM in Ba/F3 cell when use alone or combination withCetuximab(HY-P9905)[2].

体内研究
(In Vivo)

JBJ-09-063 (3 mg/kg i.v., 20 mg/kg p.o.) exhibits favorable pharmacokinetics properties and is sufficiently stable to deliver good efficacy upon oral dosing[2].

Animal Model:Mice[2]
Dosage:3 mg/kg for i.v., 20 mg/kg for p.o.
Administration:i.v. and p.o.; single dosage
Result:Pharmacokinetic Parameters of JBJ-09-063 in mice[2].
Cl (mL/min/kg), i.v.T1/2(h)Vss(L/kg)F (%)AUC 8h (ng·h/mL)
15.72.32.5152398
分子量

556.65

Formula

C31H29FN4O3S

CAS 号

2820336-67-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

溶解性数据
In Vitro: 

DMSO : 120 mg/mL(215.58 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.7965 mL8.9823 mL17.9646 mL
5 mM0.3593 mL1.7965 mL3.5929 mL
10 mM0.1796 mL0.8982 mL1.7965 mL