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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]}
批次查询： 批次纯度:

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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

 		VEGFR,mTOR 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

 		FLT3,c-Kit 85%
Linifanib ++

PDGFRβ, IC50: 66 nM

 		99%+
AZD2932 +++

PDGFRβ, IC50: 4 nM

 		c-Kit 98%
Dovitinib +++

PDGFRβ, IC50: 27 nM

 		FLT3,c-Kit 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

 		FLT3,c-Kit 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 (K650E), IC50: 4.9 nM

FGFR3, IC50: 1.0 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

 		FLT3,RET 98%
Dovitinib +++

FGFR1, IC50: 8 nM

 		+++

FGFR3, IC50: 9 nM

 		FLT3,c-Kit 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

Tags: Masitinib | 790299-79-5 | AB1010 | AB 1010 | AB-1010 | c-Kit Inhibitor | Protein Tyrosine Kinase/RTK | Apoptosis | c-Kit | PDGFR | Src | FGFR | FAK | Apoptosis | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Masitinib 纯度/质量文件 | Masitinib 亚型比较 | Masitinib 生物活性 | Masitinib 临床数据 | Masitinib 参考文献 | Masitinib 实验方案 | Masitinib 技术信息

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