您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > Entrectinib(NMS-E 628 RXDX101 ROZLYTREK)
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:
 
Entrectinib(NMS-E 628 RXDX101 ROZLYTREK)
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。
Entrectinib(NMS-E 628 RXDX101 ROZLYTREK)图片
CAS NO:1108743-60-7
规格:≥98%
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)560.64
FormulaC31H34F2N6O2
CAS No.1108743-60-7
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 100 mg/mL (178.4 mM)
Water: <1 mg/mL
Ethanol: 100 mg/mL (178.4 mM)
Other infoChemical Name: N-(5-(3,5-difluorobenzyl)-1H-indazol-3-yl)-4-(4-methylpiperazin-1-yl)-2-((tetrahydro-2H-pyran-4-yl)amino)benzamide
SMILES Code: O=C(NC1=NNC2=C1C=C(CC3=CC(F)=CC(F)=C3)C=C2)C4=CC=C(N5CCN(C)CC5)C=C4NC6CCOCC6
SynonymsEntrectinib, RXDX-101, NMS-E628; RXDX101; RXDX 101; RXDX-101; NMS E628; NMS-E-628; trade nameROZLYTREK
实验参考方法
In Vitro

In vitro activity: Entrectinib selectively blocks proliferation of ALK-dependent cell lines and potently inhibits ALK‐dependent signaling. Entrectinib also highly inhibits cell growth of the NSCLC cell line NCI‐H2228 bearing the EML4-ALK rearrangement.


Kinase Assay: Entrectinib is a potent and orally available Trk, ROS1, and ALK inhibitor; inhibits TrkA, TrkB, TrkC, ROS1 and ALK with IC50 values of 1, 3, 5, 12 and 7 nM, respectively.


Cell Assay: NLF, NLF-TrkB, SY5Y or SY5Y-TrkB cells are plated in 96 well plates, and they are exposed to drug at different concentrations (1, 5, 10, 20, 30, 50 and 100 nM of entrectinib, 1.5 μM Irino and 50 μM TMZ, respectively) for one hr followed by addition of 100 ng/mL of BDNF. Plates are harvested at 24, 48, and 72 hr following addition of drug. The plates are processed and cell viability is analyzed using a standard SRB assay protocol.

In VivoIn mice bearing Karpas-299 and SR-786 xenografts, Entrectinib (p.o.) induces complete tumor regression. In NPM-ALK transgenic mice, Entrectinib induces complete regression of tumor masses observed in the thymus and in lymph nodes. In the NB xenograft model, Entrectinib cotreatment enhanced the efficacy of conventional chemotherapy.
Animal model Mice bearing Karpas-299 and SR-786 xenograft models
Formulation & Dosage p.o. and i.v.; Entrectinib is reconstituted in 0.5% methylcellulose containing 1% Tween 80 at a final dosing volume of 10 mL/kg (e.g., 0.2 mL for a 20 gm mouse). Treatment with entrectinib, Irino and TMZ started about 15–17 days after tumor inoculation when the average tumor size is 0.2 cm3. Mice are sacrificed when tumor volume reached 3 cm3.
ReferencesExpert Opin Investig Drugs. 2015;24(11):1493-500; Cancer Res 2013;73(8 Suppl): Abstract nr 2092. doi:10.1158/1538-7445.AM2013-2092.