XL092

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

XL092  纯度: 99.52%

XL092 是一种口服有效的,ATP 竞争性的多受体酪氨酸激酶 (RTKs) 抑制剂,包括 METVEGFR2AXLMER,在细胞分析中的 IC50 值分别为 15 nM、1.6 nM、3.4 nM 和 7.2 nM。XL092 具有抗肿瘤活性。XL092 具有用于研究激酶依赖性疾病的潜力。

XL092

XL092 Chemical Structure

CAS No. : 2367004-54-2

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2330 In-stock
5 mg ¥2000 In-stock
10 mg ¥3500 In-stock
25 mg ¥7000 In-stock
50 mg ¥11000 In-stock
100 mg 询价

* Please select Quantity before adding items.

XL092 相关产品

相关化合物库:

  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Differentiation Inducing Compound Library
  • Reprogramming Compound Library
  • Orally Active Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

XL092 is an orally active, ATP-competitive inhibitor of multiple receptor tyrosine kinases (RTKs) including MET, VEGFR2, AXL and MER, with IC50s in cell-based assays of 15 nM, 1.6 nM, 3.4 nM, 7.2 nM respectively. XL092 exhibits anti-tumor activity. XL092 has the potential for kinase-dependent diseases and conditions research[1][2].

IC50 & Target[1]

MET

15 nM (IC50)

VEGFR2

1.6 nM (IC50)

AXL

3.4 nM (IC50)

MER

7.2 nM (IC50)

体内研究
(In Vivo)

XL092 (10 mg/kg/day; oral; for 14 days) causes substantial tumor growth inhibition in xenograft studies. XL092 shows 82% and 96% inhibition on p-MET and p-VEGFR2, respectively[1].
XL092 (compound 8; 3 mg/kg; iv) has a T1/2 of 5.4 hours, a CL of 43 mL/hr•kg. XL092 (3 mg/kg; po) has a T1/2 of 7.1 hours and a Cmax of 11.4 μM for rats[2].

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: Rat[1]
Dosage: 3 mg/kg (Pharmacokinetic Analysis)
Administration: IV
Result: Had a T1/2 of 5.4 hours, a CL of 43 mL/hr•kg.

Clinical Trial

分子量

528.53

Formula

C29H25FN4O5

CAS 号

2367004-54-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : 25 mg/mL (47.30 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8920 mL 9.4602 mL 18.9204 mL
5 mM 0.3784 mL 1.8920 mL 3.7841 mL
10 mM 0.1892 mL 0.9460 mL 1.8920 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    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (4.73 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (4.73 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    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: ≥ 2.08 mg/mL (3.94 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.94 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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: ≥ 2.08 mg/mL (3.94 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.94 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 20.8 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]. J. Hsu, et al. XL092, a multi-targeted inhibitor of MET, VEGFR2, AXL and MER with an optimized pharmacokinetic profile. European Journal of Cancer, Volume 138, Supplement 2, October 2020, Page S16.

    [2]. Lynne Canne Bannen, et al. Compounds for the treatment of kinase-dependent disorders. WO2019148044A1.

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