Rineterkib

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Rineterkib  纯度: 99.21%

Rineterkib (compound B) 是具有口服活性的 RAF 和ERK1/2 的抑制剂，通过激活 MAPK 通路中的突变来发挥抗增生作用。这种活性与 KRAS-突变型非小细胞肺癌、BRAF-突变型非小细胞肺癌、KRAS-突变型胰腺癌、KRAS -突变型结肠癌以及 KRAS-突变型卵巢癌尤为相关。

Rineterkib

Rineterkib Chemical Structure

CAS No. : 1715025-32-3

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2750 In-stock
5 mg ￥2500 In-stock
10 mg ￥4500 In-stock
25 mg ￥9500 In-stock
50 mg   询价  
100 mg   询价  

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Rineterkib 相关产品

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生物活性

Rineterkib (compound B) is an orally active RAF and ERK1/2 inhibitor in the study of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer[1].

IC50 & Target[1]

RAF

 

ERK1

 

ERK2

 

体内研究
(In Vivo)

Rineterkib (compound B) (50, 75 mg/kg, p.o., qd/q2d, 27 days) treatment significantly reduces the tumor volume in the Calu-6 human NSCLC subcutaneous tumor xenograft model in 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.

Animal Model: Calu-6 NSCLC xenograft tumor models in mice[1].
Dosage: 50, 75 mg/kg.
Administration: Orally either daily (qd) or every other day (q2d) for 27 days.
Result: Significantly reduced the tumor volume.

分子量

578.42

Formula

C26H27BrF3N5O2
CAS 号

1715025-32-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶解性数据
In Vitro: 

DMSO : 200 mg/mL (345.77 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7288 mL 8.6442 mL 17.2885 mL
5 mM 0.3458 mL 1.7288 mL 3.4577 mL
10 mM 0.1729 mL 0.8644 mL 1.7288 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 (sealed storage, away from moisture and light)。-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: ≥ 5 mg/mL (8.64 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (8.64 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 50.0 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

*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]. CAPONIGRO, et al. THERAPEUTIC COMBINATIONS COMPRISING A RAF INHIBITOR AND A ERK INHIBITOR. WO2018051306A1.

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