SGI-7079 | Axl Inhibitor | AmBeed-信号通路专用抑制剂

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SGI-7079 {[allProObj[0].p_purity_real_show]}

货号：A771421

SGI-7079, a selective Axl inhibitor, inhibits tumor growth in a dose dependent manner and is a potential therapeutic target for overcoming EGFR inhibitor resistance.

SGI-7079 化学结构
CAS号：1239875-86-5

SGI-7079 3D分子结构
CAS号：1239875-86-5

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SGI-7079 纯度/质量文件产品仅供科研

货号：A771421 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • JACS Au, 2024. Ambeed. [ A148168 ]; • JMC, 2024. Ambeed. [ A187643 ]; • JMC, 2024. Ambeed. [ A341145 , A633512 , A607865 , A167774 ]; • Biomacromolecules, 2024. Ambeed. [ A110759 ]; • Biomacromolecules, 2024. Ambeed. [ A203543 ]; 更多 >

VEGFR 亚型比较

产品名称	VEGFR1 ↓ ↑	VEGFR2 ↓ ↑	VEGFR3 ↓ ↑	其他靶点	纯度
Motesanib Diphosphate	++++ VEGFR1, IC50: 2 nM	++++ VEGFR2, IC50: 3 nM VEGFR2/Flk1, IC50: 3 nM	+++ VEGFR3, IC50: 6 nM	PDGFR,RET	{[allProObj[0].p_purity_real_show]}
Tivozanib	++ VEGFR1, IC50: 30 nM	+++ VEGFR2, IC50: 6.5 nM	++ VEGFR3, IC50: 15 nM		{[allProObj[0].p_purity_real_show]}
Brivanib	+ VEGFR1, IC50: 380 nM	++ VEGFR2, IC50: 25 nM Flk1, IC50: 25 nM			{[allProObj[0].p_purity_real_show]}
Regorafenib	+++ VEGFR1, IC50: 13 nM	+++ VEGFR2, IC50: 4.2 nM	+ VEGFR3, IC50: 46 nM	RET	{[allProObj[0].p_purity_real_show]}
Pazopanib	+++ VEGFR1, IC50: 10 nM	++ VEGFR2, IC50: 30 nM	+ VEGFR3, IC50: 47 nM	FGFR,PDGFR,c-Kit	{[allProObj[0].p_purity_real_show]}
Sitravatinib	+++ VEGFR1 (FLT1), IC50: 6 nM	+++ VEGFR2 (KDR), IC50: 5 nM	++++ VEGFR3 (FLT4), IC50: 2 nM		{[allProObj[0].p_purity_real_show]}
Foretinib	+++ VEGFR1/FLT1, IC50: 6.8 nM	++++ KDR, IC50: 0.86 nM	++++ VEGFR3/FLT4, IC50: 2.8 nM	Tie-2	{[allProObj[0].p_purity_real_show]}
MGCD-265 analog	++++ VEGFR1, IC50: 3 nM	++++ VEGFR2, IC50: 3 nM	++++ VEGFR3, IC50: 4 nM	Tie-2	{[allProObj[0].p_purity_real_show]}
Lactate	+++ VEGFR1/FLT1, IC50: 10 nM	+++ VEGFR2/Flk1, IC50: 13 nM	+++ VEGFR3/FLT4, IC50: 8 nM	c-Kit,FLT3	{[allProObj[0].p_purity_real_show]}
AEE788	+ FLT1, IC50: 59 nM	+ KDR, IC50: 77 nM		EGFR	{[allProObj[0].p_purity_real_show]}
Linifanib	++++ VEGFR1/FLT1, IC50: 3 nM	++++ VEGFR2/KDR, IC50: 4 nM	+ VEGFR3/FLT4, IC50: 190 nM	FLT3	{[allProObj[0].p_purity_real_show]}
Vatalanib 2HCl	+ VEGFR1/FLT1, IC50: 77 nM	++ VEGFR2/KDR, IC50: 37 nM VEGFR2/Flk1, IC50: 270 nM	+ VEGFR3/FLT4, IC50: 660 nM	c-Kit,c-Fms	{[allProObj[0].p_purity_real_show]}
Axitinib	++++ VEGFR1/FLT1, IC50: 0.1 nM	++++ VEGFR2/KDR, IC50: 0.2 nM VEGFR2/Flk1, IC50: 0.18 nM			{[allProObj[0].p_purity_real_show]}
Dovitinib	+++ VEGFR1/FLT1, IC50: 10 nM	+++ VEGFR2/Flk1, IC50: 13 nM	+++ VEGFR3/FLT4, IC50: 8 nM	c-Kit,FLT3	{[allProObj[0].p_purity_real_show]}
ZM 306416	+ VEGFR1, IC50: 0.33 μM			Src	{[allProObj[0].p_purity_real_show]}
KRN-633	+ VEGFR1, IC50: 170 nM	+ VEGFR2, IC50: 160 nM	+ VEGFR3, IC50: 125 nM	c-Kit,BTK	{[allProObj[0].p_purity_real_show]}
OSI-930	+++ FLT1, IC50: 8 nM	+++ KDR, IC50: 9 nM			{[allProObj[0].p_purity_real_show]}
Lenvatinib	++ VEGFR1/FLT1, IC50: 22 nM	++++ VEGFR2/KDR, IC50: 4.0 nM	+++ VEGFR3/FLT4, IC50: 5.2 nM		{[allProObj[0].p_purity_real_show]}
NVP-BAW2881	+ hVEGFR1, IC50: 820 nM	+++ hVEGFR2, IC50: 9 nM mVEGF2, IC50: 165 nM	+ hVEGFR3, IC50: 420 nM		{[allProObj[0].p_purity_real_show]}
Cediranib	+++ VEGFR1/FLT1, IC50: 5 nM	++++ VEGFR2/KDR, IC50: 0.5 nM		c-Kit	{[allProObj[0].p_purity_real_show]}
Nintedanib	++ VEGFR1, IC50: 34 nM	+++ VEGFR2, IC50: 13 nM	+++ VEGFR3, IC50: 13 nM	FLT3	{[allProObj[0].p_purity_real_show]}
BMS-794833		++ VEGFR2, IC50: 15 nM			{[allProObj[0].p_purity_real_show]}
SKLB1002		++ VEGFR2, IC50: 32 nM			{[allProObj[0].p_purity_real_show]}
Cabozantinib S-malate		++++ VEGFR2/KDR, IC50: 0.035 nM			{[allProObj[0].p_purity_real_show]}
Ki8751		++++ VEGFR2, IC50: 0.9 nM		c-Kit	{[allProObj[0].p_purity_real_show]}
SU 5402		++ VEGFR2, IC50: 20 nM			{[allProObj[0].p_purity_real_show]}
Rivoceranib Mesylate		++++ VEGFR2, IC50: 1 nM		RET	{[allProObj[0].p_purity_real_show]}
Ponatinib		++++ VEGFR2, IC50: 1.5 nM			{[allProObj[0].p_purity_real_show]}
LY2874455		+++ VEGFR2, IC50: 7 nM			{[allProObj[0].p_purity_real_show]}
ZM323881 HCl		++++ VEGFR2, IC50: <2 nM			{[allProObj[0].p_purity_real_show]}
AZD2932		+++ VEGFR-2, IC50: 8 nM		c-Kit	{[allProObj[0].p_purity_real_show]}
Cabozantinib		++++ VEGFR2/KDR, IC50: 0.035 nM			{[allProObj[0].p_purity_real_show]}
Sorafenib		++ VEGFR2, IC50: 90 nM VEGFR2/Flk1, IC50: 90 nM			{[allProObj[0].p_purity_real_show]}
CYC-116		++ VEGFR2, Ki: 44 nM		FLT3	{[allProObj[0].p_purity_real_show]}
Golvatinib		++ VEGFR2, IC50: 16 nM			{[allProObj[0].p_purity_real_show]}
Sunitinib		+ VEGFR2 , IC50: 80 nM		FLT3	{[allProObj[0].p_purity_real_show]}
RAF265		++ VEGFR2, EC50: 30 nM			{[allProObj[0].p_purity_real_show]}
PD173074					{[allProObj[0].p_purity_real_show]}
BFH772		++++ VEGFR2, IC50: 3 nM			{[allProObj[0].p_purity_real_show]}
Semaxinib		+ VEGFR2/Flk1, IC50: 1.23 μM			{[allProObj[0].p_purity_real_show]}
Vandetanib		++ VEGFR2, IC50: 40 nM	+ VEGFR3, IC50: 110 nM	EGFR	{[allProObj[0].p_purity_real_show]}
SAR131675			++ VEGFR3, IC50: 23 nM		{[allProObj[0].p_purity_real_show]}
ENMD-2076		+ VEGFR2/KDR, IC50: 58.2 nM	++ VEGFR3/FLT4, IC50: 15.9 nM	RET,FLT3	{[allProObj[0].p_purity_real_show]}
Telatinib		+++ VEGFR2, IC50: 6 nM	++++ VEGFR3, IC50: 4 nM	c-Kit	{[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。

SGI-7079 生物活性

描述

The AXL protein, classified as a RTK (Receptor tyrosine kinase), belongs to the TAM (TYRO3, AXL, and MER) subfamily. Overexpression or overactivation of the AXL has been correlated with the promotion of multiple tumorigenic processes. SGI-7079 is a relatively potent AXL inhibitor (IC₅₀ = 58 nM, in cell-free assays) in preclinical development. It inhibits GAS6-stimulated AXL signaling in inflammatory breast cancer cells (IC₅₀ < 1 μM), resulting in decreased cell proliferation and invasion^[3]. Mesenchymal cell lines expressing Axl were highly sensitive to SGI-7079 alone. In a mouse xenograft model of NSCLC (non-small cell lung cancer), SGI-7079 inhibited tumor growth in a dose dependent manner, and at the maximum dose, inhibited tumor growth by 67%, compared to control. Notably, SGI-7079 + erlotinib (25/100 mg/kg) reduced the tumor growth by 82%^[4].

SGI-7079 参考文献

[1]Myers SH, Brunton VG, et al. AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective. J Med Chem. 2016 Apr 28;59(8):3593-608.

[2]Byers LA, Diao L, et al. An epithelial-mesenchymal transition gene signature predicts resistance to EGFR and PI3K inhibitors and identifies Axl as a therapeutic target for overcoming EGFR inhibitor resistance. Clin Cancer Res. 2013 Jan 1;19(1):279-90.

[3]Myers SH, Brunton VG, Unciti-Broceta A. AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective. J Med Chem. 2016;59(8):3593-3608

[4]Byers LA, Diao L, Wang J, et al. An epithelial-mesenchymal transition gene signature predicts resistance to EGFR and PI3K inhibitors and identifies Axl as a therapeutic target for overcoming EGFR inhibitor resistance. Clin Cancer Res. 2013;19(1):279-290

SGI-7079 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.20mL

0.44mL

0.22mL

10.98mL

2.20mL

1.10mL

21.95mL

4.39mL

2.20mL

SGI-7079 技术信息

CAS号	1239875-86-5
分子式	C₂₆H₂₆FN₇
分子量	455.53

别名
运输	蓝冰

存储条件

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 35 mg/mL(76.83 mM)，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

SGI-7079 {[allProObj[0].p_purity_real_show]}

SGI-7079 纯度/质量文件产品仅供科研

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SGI-7079 {[allProObj[0].p_purity_real_show]}

SGI-7079 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

SGI-7079 质控信息

SGI-7079 生物活性

SGI-7079 参考文献

SGI-7079 实验方案

SGI-7079 技术信息

最近浏览的产品

大规格询价

摩尔计算器

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总药量计算器

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