Rociletinib(Synonyms: CO-1686; AVL-301; CNX-419)

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Rociletinib (Synonyms: CO-1686; AVL-301; CNX-419) 纯度: 99.79%

Rociletinib (CO-1686) 是一种可口服的 EGFR 抑制剂,能够抑制 EGFRL858R/T790M 和 EGFRWT 的活性,IC50 值分别为 21.5 nM 和 303.3 nM。

Rociletinib(Synonyms: CO-1686;  AVL-301;  CNX-419)

Rociletinib Chemical Structure

CAS No. : 1374640-70-6

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生物活性

Rociletinib (CO-1686) 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.

IC50 & Target

EGFRL858R/T790M

21.5 nM (Ki)

EGFRT790M

303.3 nM (Ki)

体外研究
(In Vitro)

Rociletinib (CO-1686) (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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Rociletinib (CO-1686) (100 mg/kg/day, p.o.) demonstrates anti-tumor activity in NSCLC EGFR mutant xenograft models. Rociletinib (CO-1686) (50 mg/kg bid, p.o.) demonstrates anti-tumor activity in human EGFR-L858R and EGFR-L858R-T790M expressing transgenic mice[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

555.55

Formula

C27H28F3N7O3

CAS 号

1374640-70-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 43 mg/mL (77.40 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8000 mL 9.0001 mL 18.0002 mL
5 mM 0.3600 mL 1.8000 mL 3.6000 mL
10 mM 0.1800 mL 0.9000 mL 1.8000 mL

*

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, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.50 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.50 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.50 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.50 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [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.

Cell Assay
[1]

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.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

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). Briefly, LUM1686 PDX tumor fragments, harvested from donor mice, are inoculated into BALB/c nude mice. Administration of test compounds (Rociletinib (CO-1686)) 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).

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [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.

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