Kobe2602

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Kobe2602  纯度: 99.55%

Kobe2602 是一个 Ras-Raf 相互作用 (Ras-Raf interaction) 抑制剂。Kobe2602 抑制 H-Ras·GTP 与 c-Raf-1 RBD 结合的 Ki 值为 149 μM。Kobe2602 具有抗肿瘤活性。

Kobe2602

Kobe2602 Chemical Structure

CAS No. : 454453-49-7

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10 mM * 1 mL in DMSO ￥1155 In-stock
50 mg ￥1050 In-stock
100 mg ￥1680 In-stock
250 mg ￥3360 In-stock
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生物活性

Kobe2602 is a Ras-Raf interaction inhibitor. Kobe2602 inhibits the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki of 149 μM. Kobe2602 has antitumor activity[1].

IC50 & Target

Ki: 149 μM (Ras-Raf interaction)[1]
体外研究
(In Vitro)

Kobe2602 (2-20 μM; 1 hour) exhibits Ras-Raf-binding inhibition in NIH 3T3 cells[1].
Kobe2602 has IC50 value of approximately 10 μM for the cellular Ras-Raf-binding inhibition[1].
Kobe2602 (20 μM) efficiently inhibits the phosphorylation of MEK and ERK, downstream kinases of Raf in NIH 3T3 cells transiently expressing H-RasG12V[1].
Kobe2602 inhibits Ras⋅GTP but not Ras⋅GDP[1].
Kobe2602 (20 μM) inhibits the anchorage-dependent proliferation of H-RasG12V-transformed cells[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.

Cell Proliferation Assay[1]

Cell Line: H-rasG12V-transformed NIH 3T3 cells
Concentration: 20 μM
Incubation Time: 24 hours , 48 hours, 72 hours
Result: Efficiently inhibited colony formation in soft agar in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: NIH 3T3 cells
Concentration: 2 μM, 20 μM
Incubation Time: 1 hour
Result: Effectively reduced the amount of c-Raf-1 associated with H-RasG12V in NIH 3T3 cells in a dose-dependent manner, indicating the inhibition of the cellular activity of Ras.

体内研究
(In Vivo)

Kobe2602 (80 mg/kg; p.o.; five consecutive days per week; for 17 days) exhibits antitumor activity on a xenograft of human colon carcinoma SW480 cells carrying the K-RasG12V gene[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: Female athymic nude mice (6-8 wk old), with SW480 cells xenograft[1]
Dosage: 80 mg/kg
Administration: Oral administration, five consecutive days per week, for 17 days
Result: Caused inhibition of the tumor growth.

分子量

419.31

Formula

C14H9F4N5O4S
CAS 号

454453-49-7
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 : 14.3 mg/mL (34.10 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3849 mL 11.9244 mL 23.8487 mL
5 mM 0.4770 mL 2.3849 mL 4.7697 mL
10 mM 0.2385 mL 1.1924 mL 2.3849 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    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 5 mg/mL (11.92 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (11.92 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 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 2.

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

    Solubility: ≥ 5 mg/mL (11.92 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (11.92 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 50.0 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]. Shima, Fumi, et al. In silico discovery of small-molecule Ras inhibitors that display antitumor activity by blocking the Ras-effector interaction. Proceedings of the National Academy of Sciences of the United States of America (2013), 110(20), 8182-8187, S8182/1-S8182/10.

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