KG5|cas:877874-85-6|西域试剂

KG5,99.79%

产品编号：Bellancom-15198| CAS NO：877874-85-6| 分子式：C₂₀H₁₆F₃N₇OS| 分子量：459.45

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货号	价格	库存与货期
Bellancom-15198	￥1400.00	杭州北京（现货）
Bellancom-15198	￥2200.00	杭州北京（现货）
Bellancom-15198	￥7800.00	杭州北京（现货）
Bellancom-15198	￥12500.00	杭州北京（现货）

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KG5

产品介绍

KG5 是一种具有口服活性的双重 PDGFRβ 和 B-Raf 变构抑制剂。KG5 还抑制 Flt3，KIT 和 c-Raf，并具有抗癌，抗血管生成活性。

生物活性

KG5 is an orally active dual PDGFRβ and B-Raf allosteric inhibitor. KG5 also inhibits Flt3, KIT and c-Raf. KG5 has anticancer, antiangiogenic activities.

体外研究

KG5 (Compound 6) inhibits vascular smooth muscle cells (VSMCs) and endothelial cells viability with EC₅₀ values of 0.59 μM and 0.54 μM, respectively.
Compound 6 selectively blocks S338 phosphorylation, yet does not influence S259.
KG5 (Compound 6) inhibits only PDGFRα and β with K_ds of 300 and 520 nM, respectively, and Flt3 and KIT at 52 and 170 nM, respectively.
KG5 (Compound 6; 5 μM) inhibits phosphorylation of MEK and ERK in endothelial cells stimulated with bFGF or VEGF.

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

体内研究

KG5 (Compound 6; 100 mg/kg; oral administration; daily; for 26 days) treatment prevents tumor growth in an orthotopic renal cell carcinoma model.
KG5 (Compound 6; 50 mg/kg; i.p.; twice daily) treatment completely blocks angiogenesis relative to vehicle control in mice (injected with Matrigel containing bFGF). Pharmacokinetic analysis of the dose and formulation of KG5 used indicated a C_max of 3.6 μg/mL, T_1/2 of 11.5 h, and an area under the concentration time curve (AUC_0-12h) of 14.7 μg•h/mL.
KG5 (Compound 6; 1 μM) disrupts a late step in angiogenesis during zebrafish embryogenesis.

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

Animal Model:	Male Nu/Nu mice injected with SN12C-RFP cells
Dosage:	100 mg/kg
Administration:	Oral administration; daily; for 26 days
Result:	Prevented tumor growth in an orthotopic renal cell carcinoma model.

体内研究

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

Animal Model:	Male Nu/Nu mice injected with SN12C-RFP cells
Dosage:	100 mg/kg
Administration:	Oral administration; daily; for 26 days
Result:	Prevented tumor growth in an orthotopic renal cell carcinoma model.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (217.65 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1765 mL	10.8826 mL	21.7652 mL
5 mM	0.4353 mL	2.1765 mL	4.3530 mL
10 mM	0.2177 mL	1.0883 mL	2.1765 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 (protect from 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 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.44 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.44 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。