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马赛替尼 /Masitinib {[allProObj[0].p_purity_real_show]}

货号:A134996 同义名: AB1010;Masican

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.

Masitinib 化学结构 CAS号:790299-79-5
Masitinib 化学结构
CAS号:790299-79-5
Masitinib 3D分子结构
CAS号:790299-79-5
Masitinib 化学结构 CAS号:790299-79-5
Masitinib 3D分子结构 CAS号:790299-79-5
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Masitinib 纯度/质量文件 产品仅供科研

货号:A134996 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 FAK 其他靶点 纯度
Defactinib 99%+
NVP-TAE 226 ++

FAK, IC50: 5.5 nM

PYK2, IC50: 3.5 nM

IGF-1R,Insulin Receptor 98+%
PF-573228 +

FAK, IC50: 4 nM

98%
Solanesol 90% +(HPLC)
PF-431396 ++

FAK, IC50: 2 nM

PYK2, IC50: 11 nM

99%+
PND-1186 ++++

FAK, IC50: 1.5 nM

99%+
PF-562271 ++++

FAK, IC50: 1.5 nM

PYK2, IC50: 13 nM

99%+
GSK2256098 ++++

FAK, Ki: 0.4 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 Fyn Lck Lyn Src Yes 其他靶点 纯度
Saracatinib ++

Fyn, IC50: 10 nM

++++

LCK, IC50: <4 nM

+++

Lyn, IC50: 5 nM

++++

c-Src, IC50: 2.7 nM

99%+
SU6656 +

Fyn, IC50: 170 nM

+

Lyn, IC50: 130 nM

+

Src, IC50: 280 nM

++

YES, IC50: 20 nM

98%
PP1 +++

Fyn, IC50: 6 nM

+++

LCK, IC50: 5 nM

EGFR 99%+
PP2 +++

Fyn, IC50: 5 nM

++++

LCK, IC50: 4 nM

98%
WH-4-023 ++++

Lck, IC50: 2 nM

+++

Src, IC50: 6 nM

99%+
NVP-BHG 712 +

c-Src, IC50: 1.266 μM

99%+
CCT196969 ++

LCK, IC50: 0.02 μM

+

Src, IC50: 0.03 μM

98%
MNS +

Src, IC50: 29.3 μM

p97,Syk 98%
Tirbanibulin ++

Src (HuH7), GI50: 13 nM

Src (Hep 3B), GI50: 26 nM

99%+
PP121 ++

Src, IC50: 14 nM

PDGFR,VEGFR 99%+
Bosutinib ++++

Src, IC50: 1.2 nM

99%
Dasatinib monohydrate ++++

Src, IC50: 0.8 nM

98%
Quercetin Sirtuin,PKC 97%
Dasatinib ++++

Src, IC50: 0.8 nM

98%
Repotrectinib +++

Src, IC50: 5.3 nM

99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 c-Kit 其他靶点 纯度
Tyrphostin AG1296 +

c-Kit (Swiss 3T3), IC50: 1.8 μM

PDGFR 99%+
Masitinib +

Kit, IC50: 200 nM

99%+
Motesanib Diphosphate +++

Kit, IC50: 8 nM

98%
Ki8751 ++

c-Kit, IC50: 40 nM

98+%
Tivozanib ++

c-Kit, IC50: 78 nM

99%+
Pazopanib +

c-Kit, IC50: 140 nM

99%
Sitravatinib +++

Kit, IC50: 6 nM

99%+
Pexidartinib +++

Kit, IC50: 10 nM

99%+
Lactate ++++

c-Kit, IC50: 2 nM

FLT3 85%
Amuvatinib +++

c-Kit (D816H), IC50: 10 nM

99%+
Imatinib Mesylate +

c-Kit, IC50: 100 nM

PDGFR 99%
AZD2932 +++

c-Kit, IC50: 9 nM

98%
Axitinib ++++

Kit, IC50: 1.7 nM

98%
Dovitinib ++++

c-Kit, IC50: 2 nM

FLT3 99%+
Sunitinib FLT3 98%
OSI-930 +

Kit, IC50: 80 nM

99%+
Telatinib ++++

c-Kit, IC50: 1 nM

99%+
Dasatinib monohydrate ++

c-Kit (wt), IC50: 79 nM

c-Kit (D816V), IC50: 37 nM

Src 98%
Dasatinib ++

c-Kit (wt), IC50: 79 nM

c-Kit (D816V), IC50: 37 nM

Src 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 PDGFR PDGFRα PDGFRβ 其他靶点 纯度
Tyrphostin A9 +

PDGFR, IC50: 0.5 μM

EGFR 98%
Tyrphostin AG1296 99%+
Motesanib Diphosphate ++

PDGFR, IC50: 84 nM

98%
Pazopanib ++

PDGFR, IC50: 84 nM

99%
Imatinib +

PDGFR, IC50: 100 nM

c-Kit 98%
Imatinib Mesylate +

PDGFR, IC50: 100 nM

c-Kit 99%
Sennoside B 99%+
PP121 ++++

PDGFR, IC50: 2 nM

mTOR,VEGFR 99%+
Crenolanib ++++

PDGFRα, Kd: 2.1 nM

++++

PDGFRβ, Kd: 3.2 nM

99%+
Masitinib +

PDGFRα, IC50: 540 nM

+

PDGFRβ, IC50: 800 nM

99%+
Ki8751 ++

PDGFRα, IC50: 67 nM

c-Kit 98+%
Tivozanib ++

PDGFRα, IC50: 40 nM

++

PDGFRβ, IC50: 49 nM

99%+
Ponatinib ++++

PDGFRα, IC50: 1.1 nM

98%
Amuvatinib ++

PDGFRα (V561D), IC50: 40 nM

99%+
Axitinib +++

PDGFRα, IC50: 5.0 nM

++++

PDGFRβ, IC50: 1.6 nM

98%
CP-673451 +++

PDGFRα, IC50: 10 nM

++++

PDGFRβ, IC50: 1 nM

99%+
Telatinib +++

PDGFRα, IC50: 15 nM

c-Kit 99%+
Nintedanib ++

PDGFRα, IC50: 59 nM

++

PDGFRβ, IC50: 65 nM

99+%
Avapritinib ++++

PDGFRα (D842V), IC50: 0.5 nM

99%+
MK-2461 +++

PDGFRβ, IC50: 22 nM

98%+
Lactate +++

PDGFRβ, IC50: 27 nM

c-Kit,FLT3 85%
Linifanib ++

PDGFRβ, IC50: 66 nM

99%+
AZD2932 +++

PDGFRβ, IC50: 4 nM

c-Kit 98%
Dovitinib +++

PDGFRβ, IC50: 27 nM

c-Kit,FLT3 99%+
Sorafenib ++

mPDGFRβ, IC50: 57 nM

PDGFRβ, IC50: 57 nM

99%
Sunitinib ++++

PDGFRβ , IC50: 2 nM

FLT3 98%
Orantinib +++

PDGFRβ, Ki: 8 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 FGFR FGFR1 FGFR2 FGFR3 FGFR4 其他靶点 纯度
Tyrphostin AG1296 +

FGFR (Swiss 3T3), IC50: 12.3 μM

PDGFR 99%+
Pazopanib +

FGFR, IC50: 140 nM

99%
Erdafitinib RET 99%+
Gambogenic acid 98+%
Sulfatinib +++

FGFR1, IC50: 15 nM

99+%
Nintedanib esylate +

FGFR1, IC50: 69 nM

++

FGFR2, IC50: 37 nM

+

FGFR3, IC50: 108 nM

98%
Zoligratinib +++

FGFR1, IC50: 9.3 nM

+++

FGFR2, IC50: 7.6 nM

++

FGFR3, IC50: 22 nM

+

FGFR4, IC50: 290 nM

99%+
MK-2461 +

FGFR1, IC50: 65 nM

++

FGFR2, IC50: 39 nM

++

FGFR3, IC50: 50 nM

98%+
SU 5402 ++

FGFR1, IC50: 30 nM

98%
Brivanib +

FGFR1, IC50: 148 nM

99%+
Lucitanib ++

FGFR1, IC50: 17.5 nM

+

FGFR2, IC50: 82.5 nM

99%+
Ponatinib ++++

FGFR1, IC50: 2.2 nM

98%
PD-166866 +

FGFR1, IC50: 52.4 nM

98%
Narazaciclib ++

FGFR1, IC50: 26 nM

RET 99%+
Lactate +++

FGFR1, IC50: 8 nM

+++

FGFR3, IC50: 9 nM

c-Kit,FLT3 85%
Lenvatinib mesylate ++

FGFR1, IC50: 46 nM

c-RET 99%
LY2874455 ++++

FGFR1, IC50: 2.8 nM

++++

FGFR2, IC50: 2.6 nM

+++

FGFR3, IC50: 6.4 nM

+++

FGFR4, IC50: 6 nM

99%+
FIIN-2 +++

FGFR1, IC50: 3.09 nM

+++

FGFR2, IC50: 4.3 nM

++

FGFR3, IC50: 27 nM

++

FGFR4, IC50: 45.3 nM

98%
FIIN-3 +++

FGFR1, IC50: 13.1 nM

++

FGFR2, IC50: 21 nM

++

FGFR3, IC50: 31.4 nM

++

FGFR4, IC50: 35.3 nM

98%
Infigratinib ++++

FGFR1, IC50: 0.9 nM

++++

FGFR2, IC50: 1.4 nM

++++

FGFR3, IC50: 1.0 nM

FGFR3 (K650E), IC50: 4.9 nM

+

FGFR4, IC50: 60 nM

99%+
Danusertib ++

FGFR1, IC50: 47 nM

RET 99%+
R1530 ++

FGFR1, IC50: 28 nM

98%
ENMD-2076 +

FGFR1, IC50: 92.7 nM

+

FGFR2, IC50: 70.8 nM

RET,FLT3 98%
Dovitinib +++

FGFR1, IC50: 8 nM

+++

FGFR3, IC50: 9 nM

c-Kit,FLT3 99%+
Sorafenib +

FGFR1, IC50: 580 nM

99%
SSR128129E +

FGFR1, IC50: 1.9 μM

99%+
AZD-4547 ++++

FGFR1, IC50: 0.2 nM

++++

FGFR2, IC50: 2.5 nM

++++

FGFR3, IC50: 1.8 nM

98%
Lenvatinib ++

FGFR1, IC50: 46 nM

RET 98%
PD173074 ++

FGFR1, IC50: ~25 nM

99%+
S49076 ++

FGFR1, IC50: 18 nM

+++

FGFR2, IC50: 17 nM

+++

FGFR3, IC50: 15 nM

98%
Futibatinib ++++

FGFR1, IC50: 1.8 nM

++++

FGFR2, IC50: 1.4 nM

++++

FGFR3, IC50: 1.6 nM

+++

FGFR4, IC50: 3.7 nM

99%+
Ferulic Acid +

FGFR1, IC50: 3.78 μM

+

FGFR2, IC50: 12.5 μM

98%
Nintedanib +

FGFR1, IC50: 69 nM

++

FGFR2, IC50: 37 nM

+

FGFR3, IC50: 108 nM

+

FGFR4, IC50: 610 nM

99+%
ASP5878 ++++

FGFR1, IC50: 0.47 nM

++++

FGFR2, IC50: 0.6 nM

++++

FGFR3, IC50: 0.74 nM

+++

FGFR4, IC50: 3.5 nM

98%
PRN1371 ++++

FGFR1, IC50: 0.6 nM

++++

FGFR2, IC50: 1.3 nM

+++

FGFR3, IC50: 4.1 nM

++

FGFR4, IC50: 19.3 nM

99%
Derazantinib +++

FGFR1, IC50: 4.5 nM

++++

FGFR2, IC50: 1.8 nM

+++

FGFR3, IC50: 4.5 nM

++

FGFR4, IC50: 34 nM

RET 99%+
ODM-203 +++

FGFR1, IC50: 11 nM

+++

FGFR2, IC50: 16 nM

+++

FGFR3, IC50: 6 nM

++

FGFR4, IC50: 35 nM

99%+
Pemigatinib ++++

FGFR1, IC50: 0.4 nM

++++

FGFR2, IC50: 0.5 nM

++++

FGFR3, IC50: 1.2 nM

++

FGFR4, IC50: 30 nM

99%+
SKLB 610 PDGFR 99%+
Alofanib 99%+
Lirafugratinib 98%
Masitinib mesylate FAK 99%+
BLU9931 +

FGFR3, IC50: 150 nM

+++

FGFR4, IC50: 3 nM

99%+
BO-264 99%+
Fisogatinib +++

FGFR4, IC50: 5 nM

99%+
H3B-6527 ++++

FGFR4, IC50: <1.2 nM

99%+
Roblitinib ++++

FGFR4, IC50: 1.9 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Masitinib 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.

Masitinib 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 - -

Masitinib 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

Masitinib 实验方案

计算器
存储液制备 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

Masitinib 技术信息

CAS号790299-79-5
分子式C28H30N6OS
分子量 498.642
别名 AB1010;Masican;Masivet.;Masitinib. Brand name: Kinavet;Masiviera
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,2-8°C

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

动物实验配方
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