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Rociletinib hydrobromide (CO-1686 (hydrobromide)) Sale

(Synonyms: CO-1686氢溴酸盐,CO-1686 hydrobromide; AVL-301 hydrobromide; CNX-419 hydrobromide) 目录号 : GC33061

Rociletinib hydrobromide (CO-1686 (hydrobromide)) (CO-1686 hydrobromide) 是一种口服激酶抑制剂,特异性靶向 EGFR 的突变形式,包括 T790M,EGFRL858R/T790M 和 EGFRWT 的 Ki 值为 21.5 nM 和 303.3 nM,分别。

Rociletinib hydrobromide (CO-1686 (hydrobromide)) Chemical Structure

Cas No.:1446700-26-0

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥630.00
现货
5mg
¥450.00
现货
10mg
¥720.00
现货
50mg
¥1,350.00
现货
100mg
¥2,250.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Cell experiment:

Cells are seeded at 3,000 cells/well in growth media supplemented with 5% FBS, 2 mM L-glutamine, and 1 % P/S, allowed to adhere overnight, and treated with a dilution series of test compound (Rociletinib) for 72 hr. Cell viability is determined by CellTiter Glo and results are represented as background-subtracted relative light units normalized to a DMSO-treated control. Growth inhibition (GI50) values are determined by GraphPad Prism 5.04. Combination index (CI) data is generated using CalcuSyn.

Animal experiment:

Briefly, NCr nu/nu mice are sub-cutaneously implanted with 1×107 tumor cells in 50% Matrigel (injection volume of 0.2 mL/mouse). Once tumors reached 100-200 mm3, Animals are dosed with compounds (Rociletinib) as outlined (N=10 animals/gp). The LUM1686 PDX xenograft study is performed by CrownBio. Briefly, LUM1686 PDX tumor fragments, harvested from donor mice, are inoculated into BALB/c nude mice. Administration of test compounds (Rociletinib) is initiated at a mean tumor size of approximately 160 mm3. Tumor growth is monitored over time to determine tumor growth inhibition of the experimental agent vs. vehicle. The endpoint of the experiment is a mean tumor volume (MTV) in control group of 2000 mm3. Percent TGI is defined as the difference between the MTV of the designated control group and the MTV of the drug-treated group, expressed as a percentage of the MTV of the designated control group. Data is presented as mean±standard error of the mean (SEM).

References:

[1]. Walter AO, et al. Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC. Cancer Discov. 2013 Sep 25.

产品描述

Rociletinib hydrobromide (CO-1686 hydrobromide) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.

Rociletinib (0.1 μM) inhibits EGFR potently and irreversibly, and inhibits more than 50% of 23 targets. Rociletinib potently and selectively inhibits growth of NSCLC cells expressing mutant EGFR and induces apoptosis. Rociletinib resistant NSCLC cell lines are sensitive to AKT inhibition[1].

Rociletinib (100 mg/kg/day, p.o.) demonstrates anti-tumor activity in NSCLC EGFR mutant xenograft models. Rociletinib (50 mg/kg bid, p.o.) demonstrates anti-tumor activity in human EGFR-L858R and EGFR-L858R-T790M expressing transgenic mice[1].

[1]. Walter AO, et al. Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC. Cancer Discov. 2013 Sep 25.

Chemical Properties

Cas No. 1446700-26-0 SDF
别名 CO-1686氢溴酸盐,CO-1686 hydrobromide; AVL-301 hydrobromide; CNX-419 hydrobromide
Canonical SMILES C=CC(NC1=CC=CC(NC2=NC(NC3=CC=C(N4CCN(C(C)=O)CC4)C=C3OC)=NC=C2C(F)(F)F)=C1)=O.[H]Br
分子式 C27H29BrF3N7O3 分子量 636.46
溶解度 DMSO : ≥ 59 mg/mL (92.70 mM) 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

制备储备液
1 mg 5 mg 10 mg
1 mM 1.5712 mL 7.856 mL 15.7119 mL
5 mM 0.3142 mL 1.5712 mL 3.1424 mL
10 mM 0.1571 mL 0.7856 mL 1.5712 mL
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