Masitinib

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Chemical Structure| 790299-79-5 同义名 : AB1010; Masican; Masiviera
CAS号 : 790299-79-5
货号 : A134996
分子式 : C28H30N6OS
纯度 : 99%+
分子量 : 498.64
MDL号 : MFCD09954132
存储条件：

Pure form Keep in dark place, sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(210.57 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • PDGFRβ

    PDGFRβ, IC50:800 nM

  • PDGFRα

    PDGFRα, IC50:540 nM

  • c-Kit

    Kit, IC50:200 nM
描述 Masitinib is an inhibitor for Kit and PDGFRα/β with IC50 of 200 nM and 540 nM/800 nM, weak inhibition to ABL and c-Fms.
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00831922 Rheumatoid Arthritis Phase 2 Completed - -
NCT00831974 Mastocytosis Phase 2 Completed - -
NCT01045577 Psoriasis Phase 2 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.01mL

0.40mL

0.20mL

10.03mL

2.01mL

1.00mL

20.05mL

4.01mL

2.01mL
参考文献

[1]Lawrence J, Saba C, et al. Masitinib demonstrates anti-proliferative and pro-apoptotic activity in primary and metastatic feline injection-site sarcoma cells. Vet Comp Oncol. 2012 Jun;10(2):143-54.

[2]Patrice D, Sebastien L, et al. Masitinib (AB1010), a Potent and Selective Tyrosine Kinase Inhibitor Targeting KIT. 2009; 4(9): e7258