TCS 359
(Synonyms: Fms-like Tyrosine Kinase Inhibitor, TCS 359) 目录号 : GC12058
A cell-permeable FLT3 inhibitor
Cas No.:301305-73-7
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
TCS 359 is a potent inhibitor against the fms-like tyrosine kinase-3 (FLT3) [1] [2] with an IC50 value of 0.042 ±0.03 µM [2].
FLT3 is a receptor tyrosine kinase. Via hematopoietic regulation, it plays its important role in the pathogenesis of acute myeloid leukemia (AML) [3].
To the proliferation of MV4-11 cell line (a human acute myeloid leukemia cell line expressing a constitutively activated mutant FLT3), the IC50 of TCS 359 was 0.34 µM [2].
TCS 359 blocked the ability of FLT3 ligand to promote the development of two-cell-embryos to the hatched blastocyst stage in mice. TCS 359 also decreased the expression of FLT3 ligand in early embryos after the four-cell stage. Without exogenous FLT3 ligand, TCS 359 did not affect embryo development [4]. Treated with another FLT3 inhibitor SU5416, 21 of 22 analyzed patients expressed FLT3 protein, 17 expressed phosphorylated FLT3 at baseline. Among these 17 patients expressed phosphorylated FLT3, inhibition of more than 50% relative to baseline was apparent in seven cases, while inhibition ranged from 20-50% relative to baseline was apparent in an additional three cases. FLT3 phosphorylation was detected in whole blood lysates in the majority of AML patients treated with SU5416. Activated FLT3 was detectable in bone marrow aspirates from approximately 50% AML patients [5].
References:
[1]. Trzci´nska-Daneluti A.M., Nguyen L., Jiang C., et al. Use of Kinase Inhibitors to Correct ΔF508-CFTR Function. Molecular & Cellular Proteomics, 2012, 11(9):745-757.
[2]. Patch R.J., Baumann C.A., Liu J., et al. Identification of 2-acylaminothiophene-3-carboxamides as potent inhibitors of FLT3. Bioorganic & Medicinal Chemistry Letters, 2006, 16: 3282-3286.
[3]. Kar R.K., Suryadevara P., Roushan R., et al. Quantifying the Structural Requirements for Designing Newer FLT3 Inhibitors. Medicinal Chemistry, 2012, 8:913-927.
[4]. Nishijima C., Kawamura K., Okamoto N., et al. Regulation of Preimplantation Embryo Development in Mice by FMS-like Tyrosine Kinase 3 Ligand. Journal of Mammalian Ova Research, 2014, 31(1):45-51.
[5]. O'Farrell A.M., Yuen H.A., Smolich B., et al. Effects of SU5416, a small molecule tyrosine kinase receptor inhibitor, on FLT3 expression and phosphorylation in patients with refractory acute myeloid leukemia. Leuk. Res., 2004, 28(7):679-89.
| Cas No. | 301305-73-7 | SDF | |
| 别名 | Fms-like Tyrosine Kinase Inhibitor, TCS 359 | ||
| 化学名 | 2-[(3,4-dimethoxybenzoyl)amino]-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide | ||
| Canonical SMILES | COC1=C(C=C(C=C1)C(=O)NC2=C(C3=C(S2)CCCC3)C(=O)N)OC | ||
| 分子式 | C18H20N2O4S | 分子量 | 360.43 |
| 溶解度 | ≥ 9mg/mL in DMSO | 储存条件 | 4°C, protect from light |
| 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.7745 mL | 13.8723 mL | 27.7446 mL |
| 5 mM | 0.5549 mL | 2.7745 mL | 5.5489 mL |
| 10 mM | 0.2774 mL | 1.3872 mL | 2.7745 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。