1. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  2. EGFR
    VEGFR
  3. BMS-690514

BMS-690514 

目录号: HY-10333 纯度: 99.89%
产品使用指南

BMS-690514是有效,有口服活性的 EGFRVEGFR 的有效抑制剂,对于EGFR,HER2和HER4的IC50 值分别为5,9和60 nM。

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BMS-690514 Chemical Structure

BMS-690514 Chemical Structure

CAS No. : 859853-30-8

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1945
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2 mg ¥1600
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5 mg ¥2400
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10 mg ¥3580
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50 mg ¥9207
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Top Publications Citing Use of Products
  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

BMS-690514 is a potent and orally active inhibitor of EGFR and VEGFR; has IC50s of 5, 20 and 60 nM for EGFR, HER 2 and HER 4, respectively.

IC50 & Target[1]

EGFR

5 nM (IC50)

HER2

20 nM (IC50)

HER4

60 nM (IC50)

体外研究
(In Vitro)

BMS-690514 targets several critical signaling pathways: human epidermal growth factor receptor (HER)/ErbB, angiogenesis signaling through VEGFR2, lymphangiogenesis through VEGFR3, and also shows activity against VEGFR1, Flt-3, and Lck. Permeability of BMS-690514 in Caco-2 cells is in the intermediate range with a moderate potential to be a P-gp substrate[2]. BMS-690514 inhibits members of the VEGFR family with IC50 values in the range of 25 to 50 nM. Non–small cell lung tumor cells with exon 19 deletion (HCC4006, HCC827, and PC9) are highly sensitive to BMS-690514, which inhibits their proliferation with IC50 values of 2 to 35 nM. Tumor cell lines with EGFR gene amplification (DiFi, NCI-H2073, A431) are also highly sensitive to inhibition by BMS-690514. Tumor cell lines that are dependent on HER2 signaling are also found to be highly sensitive to BMS-690514. Breast and gastric tumor cell lines that have HER2 gene amplification (N87, SNU-216, AU565, BT474, KPL4, and HCC202) are inhibited with IC50 values of 20 to 60 nM[1].

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

体内研究
(In Vivo)

BMS-690514 has been shown to be efficacious in a broad spectrum of tumor xenografts. At doses that are efficacious and well tolerated in the animal models, BMS-690514 inhibits tumor cell proliferation and tumor blood flow[1]. The oral bioavailability of BMS-690514 is 78% in mice, 100% in rats, 8% in monkeys, and 29% in dogs. BMS-690514 is able to cross the blood–brain barrier with a brain-to-plasma ratio of 1. The preclinical ADME properties of BMS-690514 suggest good oral bioavailability in humans and metabolism by multiple pathways including oxidation and glucuronidation[2].

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

Clinical Trial
分子量

368.43

Formula

C19H24N6O2

CAS 号
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 : ≥ 25 mg/mL (67.86 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 2.7142 mL 13.5711 mL 27.1422 mL
5 mM 0.5428 mL 2.7142 mL 5.4284 mL
10 mM 0.2714 mL 1.3571 mL 2.7142 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: ≥ 2.5 mg/mL (6.79 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.79 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 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: ≥ 2.5 mg/mL (6.79 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.79 mM,饱和度未知) 的澄清溶液。

    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 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: ≥ 2.5 mg/mL (6.79 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.79 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。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献
Animal Administration
[2]

Rats: BMS-690514 is administered to male Sprague–Dawley rats as a 10 min infusion intraarterially (IA) (1 mg/kg) or orally by gavage (10mg/kg). Vehicles used for dosing are: IA, 10mM acetate buffer (pH 5.0, 1 mL/kg) and PO, PEG400/10mM acetate buffer (pH 5.0, 2 mL/kg) (10:90). Serial plasma samples are obtained predose and at 0.17 (or 0.25 for PO), 0.5, 0.75, 1, 2, 4, 6, 8, 12, and 24 h postdose. Rats are fasted overnight and fed 4 h postdose. The brain uptake of BMS-690514 is investigated after the last dose in a 2-week toxicology study (3, 10, and 30 mg/kg/day). Brain samples are weighed and homogenized in 3 volumes of ice-chilled water. Concentrations of BMS-690514 in plasma and brain homogenates are determined by LC/MS/MS[2].

Mice: The pharmacokinetics of BMS-690514 is investigated in male balb-c mice. A total of 18 mice are divided into two groups to receive BMS-690514 as a single dose of 1mg/kg IV bolus or 5 mg/kg orally by gavage. The vehicle used for both IV (0.1mL/mouse) and PO (0.2mL/mouse) dose is Tween-80/PG/water (10:40:50). Serum concentrations of BMS-690514 are measured at 0.05 (or 0.25 for PO), 0.5, 1, 3, 6, 8, and 24 h postdose. The mice are fasted overnight and fed 6 h after dosing. Three blood samples are taken from each mouse by retro-orbital bleeding and there are three mice per time point. At the 24h time point only one sample is taken from each of the three mice. Composite serum concentration–time profiles are constructed for pharmacokinetic analysis[2].

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

参考文献

纯度: 99.89%

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BMS-690514
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HY-10333
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