Sulfatinib (HMPL-012)
(Synonyms: 5-羟基-2-甲基吲哚,HMPL-012) 目录号 : GC32805
A multi-kinase inhibitor
Cas No.:1308672-74-3
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');)
;)
Sulfatinib is a multi-kinase inhibitor.1 It inhibits the receptor tyrosine kinases VEGFR1, VEGFR2, VEGFR3, FGFR1, colony stimulating factor 1 receptor (CSF1R), tropomyosin-related kinase B (TrkB), and FMS-related tyrosine kinase 3 (FLT3; IC50s = 2, 24, 1, 15, 4, 41, and 67 nM, respectively). It is selective for these kinases over a panel of 278 kinases (IC50s = >150 nM for all).
1.Qi, C., and Xu, J.Method of treating solid tumorsWO2018090324A1(2018)
Kinase experiment: | The KDR kinase inhibition activity is tested using the the Z-lyte assay kit. The testing system contains 300 ng/mL of recombinant human KDR catalytic domain, 10 μM of ATP, 1 μM of substrate peptide, and a test compound (Sulfatinib) at a series of different concentrations in 384-well plate; total volume is 10 μL. The enzyme inhibition proceeds at room temperature (25°C), for 1 hour at room temperature on the shaker. 5 μL of stop solution is added to stop the reaction[2]. |
Animal experiment: | The phamacokinetics of Sulfatinib are studied with male ICR mice (n=6 for each group, weight 20-30g) after a single intraveneous and oral dosing at 2.5 and 10mg/kg, respectively. For i.v. dosing formulation, Sulfatinib is dissolved in DMSO (0.25%)-solutol(10%)-ethanol(10%)-physiological saline(79.75%) at the concentration of 0.25 mg/mL. And the p.o. Dosing formulation (1mg/mL) is prepared with 0.5% CMC-Na. After i.v. Or p.o. Dosing, blood samples are collected via the ophthalmic vein at 0 (pre-close), 5, 15, 30 min and 1, 1.5, 2, 4, 8, 24 h, anti-coagulated with heparin-Na. After centrifugation, plasma samples are seprated and protein precipitated with acetonitrilel containing internal standard[2]. |
References: [1]. PCT Int. Appl. (2011), WO 2011060746 A1 20110526. | |
| Cas No. | 1308672-74-3 | SDF | |
| 别名 | 5-羟基-2-甲基吲哚,HMPL-012 | ||
| Canonical SMILES | O=S(CC1=CC=CC(NC2=NC=CC(OC3=CC4=C(NC(C)=C4)C=C3)=N2)=C1)(NCCN(C)C)=O | ||
| 分子式 | C24H28N6O3S | 分子量 | 480.58 |
| 溶解度 | DMSO : ≥ 30 mg/mL (62.42 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。 |
||
| 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 | 2.0808 mL | 10.4041 mL | 20.8082 mL |
| 5 mM | 0.4162 mL | 2.0808 mL | 4.1616 mL |
| 10 mM | 0.2081 mL | 1.0404 mL | 2.0808 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet