MGCD-265 analog

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MGCD-265 analog  纯度: 98.57%

MGCD-265 analog 是一种高效的，具有口服活性的酪氨酸激酶 c-Met 和 VEGFR2 抑制剂，其 IC50 值分别为 29 nM 和 10 nM。MGCD-265 analog 具有显著的抗肿瘤活性。

MGCD-265 analog

MGCD-265 analog Chemical Structure

CAS No. : 875337-44-3

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1366 In-stock
2 mg ￥800 In-stock
5 mg ￥1200 In-stock
10 mg ￥2100 In-stock
50 mg ￥6770 In-stock
100 mg   询价  
200 mg   询价  

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生物活性

MGCD-265 analog is a potent and oral active inhibitor of c-Met and VEGFR2 tyrosine kinases, with IC50s of 29 nM and 10 nM, respectively. MGCD-265 analog has significant antitumor activity[1].

IC50 & Target[1]

VEGFR2

10 nM (IC50)

c-Met

29 nM (IC50)

体外研究
(In Vitro)

MGCD-265 analog inhibits A549 cells migration and DU145 cells scattering, with IC50s of 0.4 μM and 0.08 μM, respectively, in HGF-driven cell migration and scattering assays[1].
MGCD-265 analog inhibits HUVEC ERK phosphorylation (IC50=0.03 μM) and HUVEC proliferation (IC50=0.006 μM) in VEGF-dependent cell-based assays[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.
体内研究
(In Vivo)

MGCD-265 analog (20 mg/kg; p.o.) inhibits tumor growth inhibition on various human tumor models in mice[1].
MGCD-265 analog exhibits moderate oral bioavailability (rat 12%, dog 42%) and Cmax (rat 0.14, dog 0.21 uM/(mg/kg)) following oral administration (rat 5-25, dog 5 mg/kg)[1].
MGCD-265 analog exhibits reasonable terminal elimination half-lives (rat 1.2, dog 5.8 h) due to plasma clearance (rat 0.33, dog 1.1 L/(kg h)) following intravenous administration (rat 2.5, dog 0.8 mg/kg) [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 Sprague-Dawley rats[1]
Dosage: 2.5 mg/kg for i.v.; 5-25 mg/kg for oral (Pharmacokinetic Analysis)
Administration: Intravenous injection and oral administration
Result: Oral bioavailability (12%), Cmax (0.14 μM/(mg/kg)), T1/2 (1.2 h),
Animal Model: Male beagle dogs
Dosage: 0.8 mg/kg for i.v.; 5 mg/kg for oral (Pharmacokinetic Analysis)
Administration: Intravenous administration and oral administration
Result: Oral bioavailability (42%), Cmax (0.21 uM/(mg/kg)), T1/2 (5.8 h).

分子量

517.60

Formula

C26H20FN5O2S2
CAS 号

875337-44-3
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 : ≥ 100 mg/mL (193.20 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9320 mL 9.6600 mL 19.3199 mL
5 mM 0.3864 mL 1.9320 mL 3.8640 mL
10 mM 0.1932 mL 0.9660 mL 1.9320 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    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.75 mg/mL (5.31 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (5.31 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 27.5 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

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.75 mg/mL (5.31 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (5.31 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 27.5 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
  • 3.

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

    Solubility: ≥ 2.75 mg/mL (5.31 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (5.31 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 27.5 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]. Claridge S, et al. Discovery of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases. Bioorg Med Chem Lett. 2008 May 1;18(9):2793-8.

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