Kobe2602|cas:454453-49-7|西域试剂

Kobe2602,99.55%

产品编号：Bellancom-15717| CAS NO：454453-49-7| 分子式：C₁₄H₉F₄N₅O₄S| 分子量：419.31

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货号	价格	库存与货期
Bellancom-15717	￥1050.00	杭州北京（现货）
Bellancom-15717	￥1680.00	杭州北京（现货）
Bellancom-15717	￥3360.00	杭州北京（现货）

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Kobe2602

产品介绍

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 K_i 值为 149 μM。Kobe2602 具有抗肿瘤活性。

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 K_i of 149 μM. Kobe2602 has antitumor activity.

体外研究

Kobe2602 (2-20 μM; 1 hour) exhibits Ras-Raf-binding inhibition in NIH 3T3 cells.
Kobe2602 has IC₅₀ value of approximately 10 μM for the cellular Ras-Raf-binding inhibition.
Kobe2602 (20 μM) efficiently inhibits the phosphorylation of MEK and ERK, downstream kinases of Raf in NIH 3T3 cells transiently expressing H-Ras^G12V.
Kobe2602 inhibits Ras⋅GTP but not Ras⋅GDP.
Kobe2602 (20 μM) inhibits the anchorage-dependent proliferation of H-Ras^G12V-transformed cells.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line:	H-ras^G12V-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

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-Ras^G12V 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-Ras^G12V gene.

西域 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
Dosage:	80 mg/kg
Administration:	Oral administration, five consecutive days per week, for 17 days
Result:	Caused inhibition of the tumor growth.

体内研究

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-Ras^G12V gene.

西域 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
Dosage:	80 mg/kg
Administration:	Oral administration, five consecutive days per week, for 17 days
Result:	Caused inhibition of the tumor growth.

体内研究

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-Ras^G12V gene.

西域 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
Dosage:	80 mg/kg
Administration:	Oral administration, five consecutive days per week, for 17 days
Result:	Caused inhibition of the tumor growth.

性状

Solid

溶解性数据

In Vitro:

DMSO : 14.3 mg/mL (34.10 mM; Need ultrasonic and warming)

H₂O : < 0.1 mg/mL (insoluble)

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。