R916562
目录号 : GC33271R916562是有效的和有选择性的Axl/VEGF-R2双重抑制剂,IC50值分别为136和24nM。
Cas No.:1037798-41-6
Sample solution is provided at 25 µL, 10mM.
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- Purity: >98.00%
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Animal experiment: | Mice[1]The nu/nu mice are used in the study. In the MDA-MB-231 human breast cancer xenograft model, mice are given 125 mg/kg b.i.d. orally for 21 days. Mean tumor volume is measured[1]. |
References: [1]. Goff D, et al. Discovery of dual Axl/VEGF-R2 inhibitors as potential anti-angiogenic and anti-metastatic drugs for cancer chemotherapy. Bioorg Med Chem Lett. 2017 Aug 15; 27(16):3766-3771. |
R916562 is a potential and selective Axl/VEGF-R2 dual inhibitor with IC50s of 136 and 24 nM, respectively.
R916562 delays and inhibits tumor growth in MDA-MB-231 human breast cancer xenograft model. R916562 also shows efficacy in the Caki-1 human renal carcinoma xenograft model. R916562 treatment at 85 mg/kg or 125 mg/kg orally b.i. d for 21 days results in statistically significant tumor growth inhibitions of 69% or 83% respectively. R916562 shows 73% reduction in fibroblast growth factor-induced neovascularization in a mouse corneal micropocket assay at a dose of 100 mg/kg and 50% reduction at 50 mg/kg[1].
[1]. Goff D, et al. Discovery of dual Axl/VEGF-R2 inhibitors as potential anti-angiogenic and anti-metastatic drugs for cancer chemotherapy. Bioorg Med Chem Lett. 2017 Aug 15; 27(16):3766-3771.
Cas No. | 1037798-41-6 | SDF | |
Canonical SMILES | NC1=NC(NC(C=C2)=CC=C2N3CCN([C@H]4[C@@H]5CC[C@@H](C5)C4)CC3)=NN1C6=NC(Cl)=NC7=C6SC=C7C | ||
分子式 | C26H30ClN9S | 分子量 | 536.09 |
溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
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1 mg | 5 mg | 10 mg | |
1 mM | 1.8654 mL | 9.3268 mL | 18.6536 mL |
5 mM | 0.3731 mL | 1.8654 mL | 3.7307 mL |
10 mM | 0.1865 mL | 0.9327 mL | 1.8654 mL |
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给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
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1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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Discovery of dual Axl/VEGF-R2 inhibitors as potential anti-angiogenic and anti-metastatic drugs for cancer chemotherapy
Bioorg Med Chem Lett 2017 Aug 15;27(16):3766-3771.PMID:28711351DOI:10.1016/j.bmcl.2017.06.071
Axl tyrosine kinase has been shown to be involved in multiple pathways contributing to tumor development, angiogenesis, and metastasis. High Axl expression has been observed in many human tumors where it appears to confer aggressive tumor behavior. Here we present several series of dual Axl-VEGF-R2 kinase inhibitors based on extensive optimization of an acyl diaminotriazole. It was hypothesized that dual inhibition of these two receptor tyrosine kinases may have a synergistic affect in inhibiting tumor angiogenesis and metastasis. One of these molecules, R916562 showed comparable activity to Sunitinib in two mouse tumor xenograft models and a mouse corneal micropocket model.