TAS-115 mesylate (TAS-115 methanesulfonate)
(Synonyms: TAS-115 mesylate) 目录号 : GC33273
A multi-kinase inhibitor
Cas No.:1688673-09-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | Tumor cells (8000 cells/800 mL) with or without TAS-115 (1.0 μM) or erlotinib (0.3 μM) in the lower Transwell collagen–coated chambers are cocultured with MRC-5 (1000 cells/300 μL) cells in the upper chamber for 72 hours. The upper chamber is then removed. Cell viability is measured using the MTT assay[2]. |
Animal experiment: | Mice[1]The TAS-115 dose levels are set at 12.5, 50, and 200 mg/kg/d. The dose level for sunitinib is set at 40 mg/kg/d. Oral drug treatment is continued for 14 or 42 consecutive days for the chronic dosing in the SC-9 xenograft model. During the treatment period, TV and body weight are measured twice per week. The antitumor efficacy is assessed at the end of each study period[1]. |
References: [1]. Fujita H, et al. The novel VEGF receptor/MET-targeted kinase inhibitor TAS-115 has marked in vivo antitumor properties and a favorable tolerability profile. Mol Cancer Ther. 2013 Dec;12(12):2685-96. | |
TAS 115 is a multi-kinase inhibitor that inhibits the growth factor receptors PDGFRα and PDGFRβ (IC50s = 0.81 and 7.06 nM, respectively), c-FMS (IC50 = 15 nM), VEGFR2 and VEGFR1 (IC50s = 30 and 140 nM, respectively), Met (IC50 = 32 nM), and FGFR2 (IC50 = 340 nM).1,2 It also inhibits Axl, c-Kit, Src, and FLT1.1 TAS 115 inhibits VEGF-induced VEGFR2 phosphorylation in human umbilical vein endothelial cells (HUVECs) and Met phosphorylation in Met-amplified MKN45 human gastric cancer cells. It also inhibits VEGF-dependent, but not VEGF-independent, growth of HUVECs (IC50s = 0.019 and 19.3 ?M, respectively) and of Met-amplified MKN45, but not Met-inactivated, human MCF-7 breast cancer cells (GI50s = 0.032 and >10 ?M, respectively). TAS 115 reduces tumor growth in a MKN45 mouse xenograft model (ED50 = 8 mg/kg).
1.Fujita, H., Miyadera, K., Kato, M., et al.The novel VEGF receptor/MET-targeted kinase inhibitor TAS-115 has marked in vivo antitumor properties and a favorable tolerability profileMol. Cancer Ther.12(12)2685-2696(2013) 2.Koyama, K., Goto, H., Morizumi, S., et al.The tyrosine kinase inhibitor TAS-115 attenuates bleomycin-induced lung fibrosis in miceAm. J. Respir. Cell Mol. Biol.60(4)478-487(2019)
| Cas No. | 1688673-09-7 | SDF | |
| 别名 | TAS-115 mesylate | ||
| Canonical SMILES | CS(=O)(O)=O.O=C(C1=C(OC)C=C2N=CC=C(OC3=CC=C(NC(NC(CC4=CC=CC=C4)=O)=S)C=C3F)C2=C1)NC | ||
| 分子式 | C28H27FN4O7S2 | 分子量 | 614.66 |
| 溶解度 | DMSO : 75 mg/mL (122.02 mM) | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6269 mL | 8.1346 mL | 16.2692 mL |
| 5 mM | 0.3254 mL | 1.6269 mL | 3.2538 mL |
| 10 mM | 0.1627 mL | 0.8135 mL | 1.6269 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
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，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。