SAR131675 | VEGFR3 Inhibitor | AmBeed-信号通路专用抑制剂

SAR131675 {[allProObj[0].p_purity_real_show]}

货号：A342706

SAR131675是一种选择性的VEGFR3抑制剂，IC50为23 nM，Ki值为12 nM。

SAR131675 化学结构
CAS号：1433953-83-3

SAR131675 3D分子结构
CAS号：1433953-83-3

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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/Flk1, IC50: 3 nM VEGFR2, IC50: 3 nM	+++ VEGFR3, IC50: 6 nM	RET,PDGFR	97%
Tivozanib	++ VEGFR1, IC50: 30 nM	+++ VEGFR2, IC50: 6.5 nM	++ VEGFR3, IC50: 15 nM		99%+
Brivanib	+ VEGFR1, IC50: 380 nM	++ Flk1, IC50: 25 nM VEGFR2, 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,PDGFR,FGFR	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/Flk1, IC50: 270 nM VEGFR2/KDR, IC50: 37 nM	+ VEGFR3/FLT4, IC50: 660 nM	c-Kit,c-Fms/CSF1R	99%+
Axitinib	++++ VEGFR1/FLT1, IC50: 0.1 nM	++++ VEGFR2/Flk1, IC50: 0.18 nM VEGFR2/KDR, IC50: 0.2 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/Flk1, IC50: 90 nM VEGFR2, 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。

SAR131675 生物活性

靶点

VEGFR3

VEGFR3, IC50:23 nM

描述

One key molecule mediating tumor lymphangiogenesis is the VEGF receptor-3 (VEGFR-3), a tyrosine kinase receptor recognized and activated by VEGFC and VEGFD, commonly expressed in malignant and tumor-infiltrating stromal cells^[3]. SAR131675 is a potent and selective VEGFR-3 inhibitor which inhibits VEGFR-3 tyrosine kinase activity and VEGFR-3 autophosphorylation in HEK cells with IC₅₀ values of 20 and 45 nmol/L, respectively. SAR131675 dose dependently inhibits the proliferation of primary human lymphatic cells, induced by the VEGFR-3 ligands VEGFC and VEGFD, with an IC₅₀ of about 20 nmol/L^[3]. SAR131675 is well tolerated in mice and shows a potent antitumoral effect in several orthotopic and syngenic models, including mammary 4T1 carcinoma and RIP1.Tag2 tumors. Interestingly, it significantly reduces lymph node invasion and lung metastasis, showing its antilymphangiogenic activity in vivo. Moreover, SAR131675 significantly reduces TAM (tumor-associated macrophages) infiltration and aggregation in 4T1 tumors^[3].

SAR131675 细胞实验

Cell Line Human dermal lymphatic endothelial cells (HDLECs) Lymphatic Endothelial Cells (LECs)	Concentration	Treated Time	Description	References
Human dermal lymphatic endothelial cells (HDLECs)	10 nM or 100 nM	24 hours	To investigate the effect of VEGFR3 inhibition on LEC-conditioned medium, results showed that SAR131675 pre-treatment significantly attenuated the promotive effects of LEC-conditioned medium on cardiomyocyte hypertrophy and proliferation.	J Sport Health Sci. 2022 Jul;11(4):466-478.
Lymphatic Endothelial Cells (LECs)	30 nM		SAR131675 significantly inhibited the proliferation, migration, and tube formation of lymphatic endothelial cells but did not completely block these processes.	J Gastroenterol. 2023 Sep;58(9):908-924.

Cell Line

Human dermal lymphatic endothelial cells (HDLECs) Lymphatic Endothelial Cells (LECs)

Concentration

Treated Time

Description

References

Human dermal lymphatic endothelial cells (HDLECs)

10 nM or 100 nM

24 hours

To investigate the effect of VEGFR3 inhibition on LEC-conditioned medium, results showed that SAR131675 pre-treatment significantly attenuated the promotive effects of LEC-conditioned medium on cardiomyocyte hypertrophy and proliferation.

J Sport Health Sci. 2022 Jul;11(4):466-478.

Lymphatic Endothelial Cells (LECs)

30 nM

SAR131675 significantly inhibited the proliferation, migration, and tube formation of lymphatic endothelial cells but did not completely block these processes.

J Gastroenterol. 2023 Sep;58(9):908-924.

SAR131675 动物实验

Species Mice BALB/c mice C57BL/6J mice Mice	Animal Model ICCA xenograft model 4T1 tumor model Swimming exercise-induced physiological cardiac growth model Rotator cuff injury model	Administration	Dosage	Frequency	Description	References
Mice	ICCA xenograft model		100 mg/kg		SAR131675 significantly inhibited lymphangiogenesis in the iCCA mouse model but did not completely block it.	J Gastroenterol. 2023 Sep;58(9):908-924.
BALB/c mice	4T1 tumor model	Oral	100 mg/kg	Once daily for 10 consecutive days	To evaluate the effect of SAR131675 on tumor lymphatic vessel density in vivo, results showed that SAR131675 significantly reduced tumor lymphatic vessel density and enhanced intratumoral drug accumulation.	Signal Transduct Target Ther. 2024 Apr 15;9(1):89
C57BL/6J mice	Swimming exercise-induced physiological cardiac growth model	Oral	100 mg/kg/d	Once daily for 3 weeks	To investigate the effect of VEGFR3 inhibition on exercise-induced cardiac growth, results showed that SAR131675 significantly attenuated exercise-induced cardiac hypertrophy and proliferation, and reduced lymphatic vessel density and LYVE-1, Podoplanin expression levels in the heart.	J Sport Health Sci. 2022 Jul;11(4):466-478.
Mice	Rotator cuff injury model	Oral	50 mg/kg/day	Once daily for 2, 4, or 8 weeks	To inhibit lymphangiogenesis and evaluate its effect on rotator cuff healing. Results showed that SAR131675 significantly inhibited lymphangiogenesis in the injured area and impeded rotator cuff healing, as evidenced by lower histological scores, bone morphometric parameters, and biomechanical properties.	J Orthop Translat. 2022 Oct 21;38:65-75

Species

Mice BALB/c mice C57BL/6J mice Mice

Animal Model

ICCA xenograft model 4T1 tumor model Swimming exercise-induced physiological cardiac growth model Rotator cuff injury model

Administration

Dosage

Frequency

Description

References

Mice

ICCA xenograft model

100 mg/kg

SAR131675 significantly inhibited lymphangiogenesis in the iCCA mouse model but did not completely block it.

J Gastroenterol. 2023 Sep;58(9):908-924.

BALB/c mice

4T1 tumor model

Oral

100 mg/kg

Once daily for 10 consecutive days

To evaluate the effect of SAR131675 on tumor lymphatic vessel density in vivo, results showed that SAR131675 significantly reduced tumor lymphatic vessel density and enhanced intratumoral drug accumulation.

Signal Transduct Target Ther. 2024 Apr 15;9(1):89

C57BL/6J mice

Swimming exercise-induced physiological cardiac growth model

Oral

100 mg/kg/d

Once daily for 3 weeks

To investigate the effect of VEGFR3 inhibition on exercise-induced cardiac growth, results showed that SAR131675 significantly attenuated exercise-induced cardiac hypertrophy and proliferation, and reduced lymphatic vessel density and LYVE-1, Podoplanin expression levels in the heart.

J Sport Health Sci. 2022 Jul;11(4):466-478.

Mice

Rotator cuff injury model

Oral

50 mg/kg/day

Once daily for 2, 4, or 8 weeks

To inhibit lymphangiogenesis and evaluate its effect on rotator cuff healing. Results showed that SAR131675 significantly inhibited lymphangiogenesis in the injured area and impeded rotator cuff healing, as evidenced by lower histological scores, bone morphometric parameters, and biomechanical properties.

J Orthop Translat. 2022 Oct 21;38:65-75

SAR131675 参考文献

SAR131675 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.79mL

0.56mL

0.28mL

13.95mL

2.79mL

1.40mL

27.90mL

5.58mL

2.79mL

SAR131675 技术信息

CAS号	1433953-83-3
分子式	C₁₈H₂₂N₄O₄
分子量	358.39
SMILES Code	O=C1C(C(NC)=O)=C(N)N(CC)C2=NC(C#C[C@@](COC)(C)O)=CC=C21
MDL No.	MFCD23098773

别名
运输	蓝冰
InChI Key	PFMPOBVAYMTUOX-GOSISDBHSA-N
Pubchem ID	71295845

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

溶解方案

细胞实验：

DMSO: 105 mg/mL(292.98 mM)，配合低频超声，并水浴加热至45℃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：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

方案三

配制的工作液建议现用现配，短期内尽快用完。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

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SAR131675 参考文献

SAR131675 实验方案

SAR131675 技术信息

最近浏览的产品

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