TP-0903
(Synonyms: TP-0903) 目录号 : GC14218
An Axl kinase inhibitor
Cas No.:1341200-45-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Description:
IC50: 0.027 μM against AXL
AXL and other TAM family members are known to be involved in maintaining the mesenchymal phenotype in cancer cells. Mesenchymal cells have increased invasion and migratory properties, enhanced cell survival in stressed environments, as well as increased resistance to targeted therapies. TP-0903 is a potent anti-cancer agent targeting the AXL receptor tyrosine kinase.
In vitro: On the basis of the potency of TP-0903 in biochemical assays, its activity in cell-based studies was evaluated. TP-0903 showed extremely potent activity in cell viability assays against the pancreatic cancer cell line PSN-1. More importantly, TP-0903 was evaluated for its ability to block GAS6-mediated activation of AXL in pancreatic cancer cells. PSN-1 cells were serum-starved and then stimulated with GAS6 in the presence of various concentrations of TP-0903 [1].
In vivo: TP-0903 restores sensitivity to erlotinib in cell-based and preclinical animal models of cancer by reversing the mesenchymal phenotype driving resistance [2].
Clinical trial: Up to now, TP-0903 is still in the preclinical development stage.
Reference:
[1] Mollard A, Warner SL, Call LT, Wade ML, Bearss JJ, Verma A, Sharma S, Vankayalapati H, Bearss DJ. Design, Synthesis and Biological Evaluation of a Series of Novel Axl Kinase Inhibitors. ACS Med Chem Lett. 2011 Dec 8;2(12):907-912.
[2] ToleroPharmaceuticals, Inc–TP-0903. http://www.toleropharmaceuticals.com/TP-0903.html.
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9378 mL | 9.6888 mL | 19.3776 mL |
| 5 mM | 0.3876 mL | 1.9378 mL | 3.8755 mL |
| 10 mM | 0.1938 mL | 0.9689 mL | 1.9378 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。
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