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Amuvatinib {[allProObj[0].p_purity_real_show]}

货号：A205668 同义名： MP470;HPK 56 Ambeed 开学季，买赠积分，赢豪礼

Amuvatinib is a potent and multi-targeted inhibitor that inhibits c-Kit, PDGFRα and Flt3 with IC50 of 10, 40 and 81 nM respectively.

Amuvatinib 化学结构 CAS号：850879-09-3
Amuvatinib 化学结构
CAS号：850879-09-3
Amuvatinib 3D分子结构
CAS号：850879-09-3
Amuvatinib 化学结构 CAS号：850879-09-3
Amuvatinib 3D分子结构 CAS号：850879-09-3
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Amuvatinib 纯度/质量文件 产品仅供科研

货号：A205668 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 c-Kit ↓ 其他靶点 纯度
Tyrphostin AG1296 +

c-Kit (Swiss 3T3), IC50: 1.8 μM

 		PDGFR {[allProObj[0].p_purity_real_show]}
Masitinib +

Kit, IC50: 200 nM

 		{[allProObj[0].p_purity_real_show]}
Motesanib Diphosphate +++

Kit, IC50: 8 nM

 		{[allProObj[0].p_purity_real_show]}
Ki8751 ++

c-Kit, IC50: 40 nM

 		{[allProObj[0].p_purity_real_show]}
Tivozanib ++

c-Kit, IC50: 78 nM

 		{[allProObj[0].p_purity_real_show]}
Pazopanib +

c-Kit, IC50: 140 nM

 		{[allProObj[0].p_purity_real_show]}
Sitravatinib +++

Kit, IC50: 6 nM

 		{[allProObj[0].p_purity_real_show]}
Pexidartinib +++

Kit, IC50: 10 nM

 		{[allProObj[0].p_purity_real_show]}
Lactate ++++

c-Kit, IC50: 2 nM

 		FLT3 {[allProObj[0].p_purity_real_show]}
Amuvatinib +++

c-Kit (D816H), IC50: 10 nM

 		{[allProObj[0].p_purity_real_show]}
Imatinib Mesylate +

c-Kit, IC50: 100 nM

 		PDGFR {[allProObj[0].p_purity_real_show]}
AZD2932 +++

c-Kit, IC50: 9 nM

 		{[allProObj[0].p_purity_real_show]}
Axitinib ++++

Kit, IC50: 1.7 nM

 		{[allProObj[0].p_purity_real_show]}
Dovitinib ++++

c-Kit, IC50: 2 nM

 		FLT3 {[allProObj[0].p_purity_real_show]}
Sunitinib ✔ FLT3 {[allProObj[0].p_purity_real_show]}
OSI-930 +

Kit, IC50: 80 nM

 		{[allProObj[0].p_purity_real_show]}
Telatinib ++++

c-Kit, IC50: 1 nM

 		{[allProObj[0].p_purity_real_show]}
Dasatinib monohydrate ++

c-Kit (wt), IC50: 79 nM

c-Kit (D816V), IC50: 37 nM

 		Src {[allProObj[0].p_purity_real_show]}
Dasatinib ++

c-Kit (wt), IC50: 79 nM

c-Kit (D816V), IC50: 37 nM

 		Src {[allProObj[0].p_purity_real_show]}
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 {[allProObj[0].p_purity_real_show]}
Tyrphostin AG1296 {[allProObj[0].p_purity_real_show]}
Motesanib Diphosphate ++

PDGFR, IC50: 84 nM

 		{[allProObj[0].p_purity_real_show]}
Pazopanib ++

PDGFR, IC50: 84 nM

 		{[allProObj[0].p_purity_real_show]}
Imatinib +

PDGFR, IC50: 100 nM

 		c-Kit {[allProObj[0].p_purity_real_show]}
Imatinib Mesylate +

PDGFR, IC50: 100 nM

 		c-Kit {[allProObj[0].p_purity_real_show]}
Sennoside B ✔ {[allProObj[0].p_purity_real_show]}
PP121 ++++

PDGFR, IC50: 2 nM

 		mTOR,VEGFR {[allProObj[0].p_purity_real_show]}
Crenolanib ++++

PDGFRα, Kd: 2.1 nM

 		++++

PDGFRβ, Kd: 3.2 nM

 		{[allProObj[0].p_purity_real_show]}
Masitinib +

PDGFRα, IC50: 540 nM

 		+

PDGFRβ, IC50: 800 nM

 		{[allProObj[0].p_purity_real_show]}
Ki8751 ++

PDGFRα, IC50: 67 nM

 		c-Kit {[allProObj[0].p_purity_real_show]}
Tivozanib ++

PDGFRα, IC50: 40 nM

 		++

PDGFRβ, IC50: 49 nM

 		{[allProObj[0].p_purity_real_show]}
Ponatinib ++++

PDGFRα, IC50: 1.1 nM

 		{[allProObj[0].p_purity_real_show]}
Amuvatinib ++

PDGFRα (V561D), IC50: 40 nM

 		{[allProObj[0].p_purity_real_show]}
Axitinib +++

PDGFRα, IC50: 5.0 nM

 		++++

PDGFRβ, IC50: 1.6 nM

 		{[allProObj[0].p_purity_real_show]}
CP-673451 +++

PDGFRα, IC50: 10 nM

 		++++

PDGFRβ, IC50: 1 nM

 		{[allProObj[0].p_purity_real_show]}
Telatinib +++

PDGFRα, IC50: 15 nM

 		c-Kit {[allProObj[0].p_purity_real_show]}
Nintedanib ++

PDGFRα, IC50: 59 nM

 		++

PDGFRβ, IC50: 65 nM

 		{[allProObj[0].p_purity_real_show]}
Avapritinib ++++

PDGFRα (D842V), IC50: 0.5 nM

 		{[allProObj[0].p_purity_real_show]}
MK-2461 +++

PDGFRβ, IC50: 22 nM

 		{[allProObj[0].p_purity_real_show]}
Lactate +++

PDGFRβ, IC50: 27 nM

 		FLT3,c-Kit {[allProObj[0].p_purity_real_show]}
Linifanib ++

PDGFRβ, IC50: 66 nM

 		{[allProObj[0].p_purity_real_show]}
AZD2932 +++

PDGFRβ, IC50: 4 nM

 		c-Kit {[allProObj[0].p_purity_real_show]}
Dovitinib +++

PDGFRβ, IC50: 27 nM

 		FLT3,c-Kit {[allProObj[0].p_purity_real_show]}
Sorafenib ++

PDGFRβ, IC50: 57 nM

mPDGFRβ, IC50: 57 nM

 		{[allProObj[0].p_purity_real_show]}
Sunitinib ++++

PDGFRβ , IC50: 2 nM

 		FLT3 {[allProObj[0].p_purity_real_show]}
Orantinib +++

PDGFRβ, Ki: 8 nM

 		{[allProObj[0].p_purity_real_show]}
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 FLT3 ↓ 其他靶点 纯度
R406 ✔ Syk {[allProObj[0].p_purity_real_show]}
Go6976 ✔ {[allProObj[0].p_purity_real_show]}
Quizartinib +++

FLT3 (ITD), IC50: 1.1 nM

FLT3 (WT), IC50: 4.2 nM

 		{[allProObj[0].p_purity_real_show]}
Gilteritinib ++++

FLT3, IC50: 0.29 nM

 		{[allProObj[0].p_purity_real_show]}
Amuvatinib +

FLT3 (D835Y), IC50: 81 nM

 		{[allProObj[0].p_purity_real_show]}
Pacritinib ++

FLT3 (D835Y), IC50: 6 nM

FLT3, IC50: 22 nM

 		{[allProObj[0].p_purity_real_show]}
Dovitinib ++++

FLT3, IC50: 1 nM

 		c-Kit {[allProObj[0].p_purity_real_show]}
Denfivontinib ++++

FLT3 (D835Y), IC50: 0.4 nM

FLT3, IC50: 0.4 nM

 		RET {[allProObj[0].p_purity_real_show]}
TAK-659 HCl ++

FLT3, IC50: 4.6 nM

 		Syk {[allProObj[0].p_purity_real_show]}
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。

Amuvatinib 生物活性

靶点

  • PDGFRα

    PDGFRα (V561D), IC50:40 nM

  • c-Kit

    c-Kit (D816H), IC50:10 nM

  • FLT3

    FLT3 (D835Y), IC50:81 nM
描述 c-KIT is a tyrosine-protein kinase that acts as cell-surface receptor for the cytokine KITLG/SCF and plays an essential role in the regulation of cell survival and proliferation, hematopoiesis, stem cell maintenance, gametogenesis, mast cell development, migration and function, and in melanogenesis. c-KIT is a proto-oncogene. Activating or gain of function mutations in c-KIT have been identified in a variety of tumors[3]. Amuvatinib, also termed MP470, is an inhibitor of various mutant c-KIT kinases. The inhibitory IC50s of MP470 against c-KIT(D816V), c-KIT(D816H), c-KIT(V560G), c-KIT(V654A) were 0.95 μM, 0.01 μM, 0.034 μM and 0.127 μM, respectively. The IC50 for MP470 on OVCAR-3 cells proliferation was 0.9 μM[3]. According to another report, the IC50 for MP470 on prostate cancer LNCaP and PC-3 cells were ~4 μM and 8 μM, respectively, when incubated for 4 days. Flow cytometric analysis revealed that 48h treatment of MP470 to LNCaP cells at the concentration of 10 μM induced 28% of apoptosis[4]. In a HT-29 xenograft model, MP470 was i.p. administrated at the doses of 10 or 20 mg/kg at the schedule of 5 times a week for 2 weeks. Both doses significantly inhibited tumor growth. In an A549 xenograft model, MP470 was orally administrated at the doses of 50, 100, or 200 mg/kg, also 5 times a week for 2 weeks. All three doses exhibited anti-tumor activity[3]. In another LNCaP xenograft model, MP470 was i.p. dosed at 50 mg/kg daily for 24 days. This dose in combination with Erlotinib had a marked effect with tumor growth inhibition of 45-65%, while both drugs were of modest activity as a single agent[4].

Amuvatinib 动物研究

Dose Mice: 50 mg/kg[1] (i.p.)
Administration i.p.

Amuvatinib 参考文献

[1]Qi W, Cooke LS, et al. MP470, a novel receptor tyrosine kinase inhibitor, in combination with Erlotinib inhibits the HER family/PI3K/Akt pathway and tumor growth in prostate cancer. BMC Cancer. 2009 May 11;9:142.

[2]Mahadevan D, Cooke L, et al. A novel tyrosine kinase switch is a mechanism of imatinib resistance in gastrointestinal stromal tumors. Oncogene. 2007 Jun 7;26(27):3909-19.

[3]PHARMACEUTICAL FORMULATIONS COMPRISING SALTS OF A PROTEIN KINASE INHIBITOR AND METHODS OF USING SAME

[4]Qi W, Cooke LS, Stejskal A, Riley C, Croce KD, Saldanha JW, Bearss D, Mahadevan D. MP470, a novel receptor tyrosine kinase inhibitor, in combination with Erlotinib inhibits the HER family/PI3K/Akt pathway and tumor growth in prostate cancer. BMC Cancer. 2009 May 11;9:142.

Amuvatinib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.23mL

0.45mL

0.22mL

11.17mL

2.23mL

1.12mL

22.35mL

4.47mL

2.23mL

Amuvatinib 技术信息

CAS号850879-09-3
分子式C23H21N5O3S
分子量 447.51
别名 MP470;HPK 56
运输蓝冰
存储条件

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度

DMSO: 50 mg/mL(111.73 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

5%DMSO+95% Corn oil 4.5 mg/mL

Tags: Amuvatinib | 850879-09-3 | MP470 | HPK 56 | MP 470 | MP-470 | HPK56 | HPK 56 | HPK-56 | RTK Inhibitor | Protein Tyrosine Kinase/RTK | Cell Cycle/DNA Damage | Apoptosis | c-Kit | PDGFR | RAD51 | FLT3 | c-Met/HGFR | RET | Apoptosis | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Amuvatinib 纯度/质量文件 | Amuvatinib 亚型比较 | Amuvatinib 生物活性 | Amuvatinib 动物研究 | Amuvatinib 参考文献 | Amuvatinib 实验方案 | Amuvatinib 技术信息

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