Masitinib (AB1010)是一种新型的Kit和PDGFRα/β抑制剂,IC50分别为200 nM和540 nM/800 nM,但对ABL和c-Fms抑制作用较弱。Phase 2/3。
别名:AB1010
Masitinib (AB1010)是一种新型的Kit和PDGFRα/β抑制剂,IC50分别为200 nM和540 nM/800 nM,但对ABL和c-Fms抑制作用较弱。Phase 2/3。Masitinib浓度≤500 nM时为ATP竞争性抑制剂。Masitinib也有效抑制重组PDGFR和胞内激酶Lyn, 及FGFR 3。 然而, Masitinib 对ABL和c-Fms抑制效果很弱。
bioRxiv. 2021 May 23;445261.
Non-coding NFKBIZ 3′ UTR mutations promote cell growth and resistance to targeted therapeutics in diffuse large B-cell lymphoma
Masitinib购买自AbMole
Blood. 2018 May 24;131(21):2345-2356.
Pan-SRC kinase inhibition blocks B-cell receptor oncogenic signaling in non-Hodgkin lymphoma.
Masitinib购买自AbMole
细胞实验 | |
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细胞系 | Ba/F3 cell |
方法 | For the assay of Ba/F3 cell proliferation, microtitre plates were seeded with a total of 104 cells/well in 100 µl of RPMI 1640 medium with 10% foetal bovine serum at 37°C. These were supplemented, or not, with either 0.1% conditioned medium from X63-IL-3 cells or 250 ng/ml murine SCF. The murine SCF, which activates KIT, was purified from the conditioned medium of SCF-producing CHO cells (gift of S. Lyman, Immunex). Cells were grown for 48 hours at 37°C and then incubated with 10 µl/well of WST-1 reagent (Roche Applied Science, France) for 3 hours at 37°C. The amount of formazan dye formed was quantified by its absorbance at 450 nm using a scanning multiwell spectrophotometer (MultiSkan MS, Thermo-LabSystems, France). A blank well without cells was used as a background control for the spectrophotometer and all assays were performed in triplicate. |
浓度 | 0~10 μM |
处理时间 | 48 h |
动物实验 | |
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动物模型 | Ba/F3 Δ27 tumour model in Female MBRI Nu/Nu mice |
配制 | placebo |
剂量 | 10, 30, or 45 mg/kg twice daily for 10 days |
给药处理 | orally |
分子量 | 498.64 |
分子式 | C28H30N6OS |
CAS号 | 790299-79-5 |
溶解性(25°C) | DMSO ≥100 mg/mL |
储存条件 |
粉末型式 -20°C 3年;4°C 2年 溶于溶剂 -80°C 6个月;-20°C 1个月 |
运输方式 | 冰袋运输,根据产品的不同,可能会有相应调整。 |
以下数据基于产品分子量,对于具体产品,请根据在不同溶剂中的溶解度和COA中的说明进行操作。
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.0055 mL | 10.0273 mL | 20.0545 mL |
5 mM | 0.4011 mL | 2.0055 mL | 4.0109 mL |
10 mM | 0.2005 mL | 1.0027 mL | 2.0055 mL |
小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 | |
重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km 系数 | 3 | 6 | 12 | 8 | 5 | 20 |
动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
动物 A的Km系数 |
例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。
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Toceranib phosphate is a multitargeted indolinone receptor tyrosine kinase (RTK) inhibitor with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. |
Seralutinib (GB002)
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SU5204
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CS-2660 (JNJ-38158471)
CS-2660 (JNJ-38158471) is a well tolerated, orally available, highly selective VEGFR-2 inhibitor with IC50 of 40 nM. CS-2660 (JNJ-38158471) also inhibits closely related tyrosine kinases such as Ret and Kit with IC50 of 180 nM and 500 nM,while it has no significant activity (>1 microM) against VEGFR-1 and VEGFR-3. |
Vorolanib (X-82)
Vorolanib is an oral, multikinase, dual inhibitor of vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR) with antiangiogenic and antineoplastic activities. |
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