BFH772|cas:890128-81-1|西域试剂

BFH772,96.25%

产品编号：Bellancom-100419| CAS NO：890128-81-1| 分子式：C₂₃H₁₆F₃N₃O₃| 分子量：439.39

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货号	价格	库存与货期
Bellancom-100419	￥760.00	杭州北京（现货）
Bellancom-100419	￥1300.00	杭州北京（现货）
Bellancom-100419	￥2500.00	杭州北京（现货）
Bellancom-100419	￥3700.00	杭州北京（现货）
Bellancom-100419	￥6900.00	杭州北京（现货）

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BFH772

产品介绍

BFH772 是一种有效的，具有口服活性的 VEGFR2 抑制剂，IC₅₀ 为 3 nM。

生物活性

BFH772 is a potent oral VEGFR2 inhibitor, which is highly effective at targeting VEGFR2 kinase with an IC₅₀ value of 3 nM.

体外研究

BFH772 is highly selective; apart from inhibiting VEGFR2 at 3 nM IC₅₀, it also targets B-RAF, RET, and TIE-2, albeit with at least 40-fold lower potency. BFH772 is inactive (IC₅₀>10 μM; >2 μM for cKIT) against all other tyrosine specific- and serine/threonine-specific protein kinases tested. BFH772 inhibits VEGFR2 with IC₅₀ of 4.6±0.6 nM in CHO cells. BFH772 inhibits VEGFR2 with IC₅₀ of 3 nM in HUVEC cells. BFH772 inhibits the ligand induced autophosphorylation of RET, PDGFR, and KIT kinases, with IC₅₀ values ranging between 30 and 160 nM. BFH772 is selective (IC₅₀ values >0.5 μM) against the kinases of EGFR, ERBB2, INS-R, and IGF-1R and against the cytoplasmic BCR-ABL kinase. IC₅₀ of BFH772 (<0.01 nM, n=2) demonstrates that they abrogated VEGF induced proliferation at remarkably low nM concentrations.

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

体内研究

BFH772 at 3 mg/kg orally dosed once per day potently inhibits melanoma growth (by 54-90% for primary tumor and 71-96% for metastasis growth) as depicted by treatment to control ratios. Dose–response curves of BFH772 at 0.3, 1, and 3 mg/kg demonstrate that even at the lowest concentrations, this naphthalene-1-carboxamide inhibits VEGF induced tissue weight and TIE-2 levels but only reaches statistical significance at 1 mg/kg and above.

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (227.59 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2759 mL	11.3794 mL	22.7588 mL
5 mM	0.4552 mL	2.2759 mL	4.5518 mL
10 mM	0.2276 mL	1.1379 mL	2.2759 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% corn oil
Solubility: ≥ 2.5 mg/mL (5.69 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.69 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。