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 是一种选择性、ATP 竞争性的口服 Axl 受体酪氨酸激酶抑制剂，能够阻断 Axl 介导的 NF-κB 激活和 MMP-9 表达，从而抑制肿瘤细胞的增殖、迁移和侵袭。其体外 IC50为 58 nM，具有克服 EGFR 抑制剂耐药性的潜力。

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: • Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]; • Cell, 2025. Ambeed. [ A122167 ]; • Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]; • Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]; • Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]; 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	97%
Tivozanib	++ VEGFR1, IC50: 30 nM	+++ VEGFR2, IC50: 6.5 nM	++ VEGFR3, IC50: 15 nM		99%+
Brivanib	+ VEGFR1, IC50: 380 nM	++ VEGFR2, IC50: 25 nM Flk1, IC50: 25 nM			99%+
Regorafenib	+++ VEGFR1, IC50: 13 nM	+++ VEGFR2, IC50: 4.2 nM	+ VEGFR3, IC50: 46 nM	RET	98%
Pazopanib	+++ VEGFR1, IC50: 10 nM	++ VEGFR2, IC50: 30 nM	+ VEGFR3, IC50: 47 nM	c-Kit,FGFR,PDGFR	99%
Sitravatinib	+++ VEGFR1 (FLT1), IC50: 6 nM	+++ VEGFR2 (KDR), IC50: 5 nM	++++ VEGFR3 (FLT4), IC50: 2 nM		99%+
Foretinib	+++ VEGFR1/FLT1, IC50: 6.8 nM	++++ KDR, IC50: 0.86 nM	++++ VEGFR3/FLT4, IC50: 2.8 nM	Tie-2	99%+
MGCD-265 analog	++++ VEGFR1, IC50: 3 nM	++++ VEGFR2, IC50: 3 nM	++++ VEGFR3, IC50: 4 nM	Tie-2	99%+
Lactate	+++ VEGFR1/FLT1, IC50: 10 nM	+++ VEGFR2/Flk1, IC50: 13 nM	+++ VEGFR3/FLT4, IC50: 8 nM	FLT3,c-Kit	85%
AEE788	+ FLT1, IC50: 59 nM	+ KDR, IC50: 77 nM		EGFR	98+%
Linifanib	++++ VEGFR1/FLT1, IC50: 3 nM	++++ VEGFR2/KDR, IC50: 4 nM	+ VEGFR3/FLT4, IC50: 190 nM	FLT3	99%+
Vatalanib 2HCl	+ VEGFR1/FLT1, IC50: 77 nM	++ VEGFR2/KDR, IC50: 37 nM VEGFR2/Flk1, IC50: 270 nM	+ VEGFR3/FLT4, IC50: 660 nM	c-Fms/CSF1R,c-Kit	99%+
Axitinib	++++ VEGFR1/FLT1, IC50: 0.1 nM	++++ VEGFR2/KDR, IC50: 0.2 nM VEGFR2/Flk1, IC50: 0.18 nM			98%
Dovitinib	+++ VEGFR1/FLT1, IC50: 10 nM	+++ VEGFR2/Flk1, IC50: 13 nM	+++ VEGFR3/FLT4, IC50: 8 nM	FLT3,c-Kit	99%+
ZM 306416	+ VEGFR1, IC50: 0.33 μM			Src	99%+
KRN-633	+ VEGFR1, IC50: 170 nM	+ VEGFR2, IC50: 160 nM	+ VEGFR3, IC50: 125 nM	BTK,c-Kit	98%
OSI-930	+++ FLT1, IC50: 8 nM	+++ KDR, IC50: 9 nM			99%+
Lenvatinib	++ VEGFR1/FLT1, IC50: 22 nM	++++ VEGFR2/KDR, IC50: 4.0 nM	+++ VEGFR3/FLT4, IC50: 5.2 nM		98%
NVP-BAW2881	+ hVEGFR1, IC50: 820 nM	+++ mVEGF2, IC50: 165 nM hVEGFR2, IC50: 9 nM	+ hVEGFR3, IC50: 420 nM		99%
Cediranib	+++ VEGFR1/FLT1, IC50: 5 nM	++++ VEGFR2/KDR, IC50: 0.5 nM		c-Kit	99%+
Nintedanib	++ VEGFR1, IC50: 34 nM	+++ VEGFR2, IC50: 13 nM	+++ VEGFR3, IC50: 13 nM	FLT3	99+%
BMS-794833		++ VEGFR2, IC50: 15 nM			99%+
SKLB1002		++ VEGFR2, IC50: 32 nM			99%
Cabozantinib S-malate		++++ VEGFR2/KDR, IC50: 0.035 nM			99+%
Ki8751		++++ VEGFR2, IC50: 0.9 nM		c-Kit	99%
SU 5402		++ VEGFR2, IC50: 20 nM			98%
Apatinib mesylate		++++ VEGFR2, IC50: 1 nM		RET	98+%
Ponatinib		++++ VEGFR2, IC50: 1.5 nM			98%
LY2874455		+++ VEGFR2, IC50: 7 nM			99%+
ZM323881 HCl		++++ VEGFR2, IC50: <2 nM			98%
AZD2932		+++ VEGFR-2, IC50: 8 nM		c-Kit	99%
Cabozantinib		++++ VEGFR2/KDR, IC50: 0.035 nM			98%
Sorafenib		++ VEGFR2, IC50: 90 nM VEGFR2/Flk1, IC50: 90 nM			99%
CYC-116		++ VEGFR2, Ki: 44 nM		FLT3	99%+
Golvatinib		++ VEGFR2, IC50: 16 nM			99%+
Sunitinib		+ VEGFR2 , IC50: 80 nM		FLT3	98%
RAF265		++ VEGFR2, EC50: 30 nM			99%+
PD173074					99%+
BFH772		++++ VEGFR2, IC50: 3 nM			98%
Semaxinib		+ VEGFR2/Flk1, IC50: 1.23 μM			98%
Vandetanib		++ VEGFR2, IC50: 40 nM	+ VEGFR3, IC50: 110 nM	EGFR	99%
SAR131675			++ VEGFR3, IC50: 23 nM		99%+
ENMD-2076		+ VEGFR2/KDR, IC50: 58.2 nM	++ VEGFR3/FLT4, IC50: 15.9 nM	FLT3,RET	98%
Telatinib		+++ VEGFR2, IC50: 6 nM	++++ VEGFR3, IC50: 4 nM	c-Kit	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。

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 细胞实验

Cell Line H460 cells A549 cells KPL-4 cells SUM149 cells	Concentration	Treated Time	Description	References
H460 cells	0.1 µM	48 hours	Co-inhibition of AXL and SRC effectively blocked KRAS activity and promoted cell death	Cancers (Basel). 2025 Feb 1;17(3):490.
A549 cells	0.1 µM	48 hours	Co-inhibition of AXL and SRC effectively blocked KRAS activity and promoted cell death	Cancers (Basel). 2025 Feb 1;17(3):490.
KPL-4 cells	0.16 µM	72 hours	Inhibited the proliferation of KPL-4 cells with an IC50 of 0.16 µM.	Cancer Res. 2013 Nov 1;73(21):6516-25.
SUM149 cells	0.43 µM	72 hours	Inhibited the proliferation of SUM149 cells with an IC50 of 0.43 µM.	Cancer Res. 2013 Nov 1;73(21):6516-25.

SGI-7079 动物实验

Species Nude mice Mice	Animal Model A549 xenograft model A549 xenograft model	Administration	Dosage	Frequency	Description	References
Nude mice	A549 xenograft model	Oral	25 mg/kg	5 days a week, continuous treatment	Dual inhibition of AXL and SRC significantly suppressed tumor growth	Cancers (Basel). 2025 Feb 1;17(3):490.
Mice	A549 xenograft model		25/100 mg/kg		To test the inhibitory effect of SGI-7079 alone or in combination with erlotinib on tumor growth	Clin Cancer Res. 2013 Jan 1;19(1):279-90

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
SMILES Code	N#CCC1=CC=CC(C2=C3C(NC=C3C)=NC(NC4=CC=C(N5CCN(C)CC5)C(F)=C4)=N2)=C1
MDL No.	MFCD28963942

别名
运输	蓝冰
InChI Key	BCFKACXAIBEPKR-UHFFFAOYSA-N
Pubchem ID	46870258

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C

溶解方案

细胞实验：

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：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

方案二

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

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SGI-7079 细胞实验

SGI-7079 动物实验

SGI-7079 参考文献

SGI-7079 实验方案

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SGI-7079 纯度/质量文件 产品仅供科研

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SGI-7079 质控信息

SGI-7079 生物活性

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SGI-7079 参考文献

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