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(Rac)-SAR131675

Catalog No. T3691 CAS 1092539-44-0

Synonyms: SAR131675

(Rac)-SAR131675 is an effective and specific VEGFR-3 inhibitor. It inhibited VEGFR-3 tyrosine kinase activity (IC50: 20 nmol/L) and VEGFR-3 autophosphorylation (IC50: 45 nmol/L) in HEK cells, respectively. SAR131675 is highly specific for VEGFR-3 versus 107 receptors, enzymes, ion channels, and 65 kinases. SAR131675 is a highly specific VEGFR-3-TK inhibitor with significant antitumoral and antimetastatic activities in vivo through inhibition of lymphangiogenesis and TAM invasion.

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(Rac)-SAR131675, CAS 1092539-44-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 50.00
5 mg	In stock	$ 113.00
10 mg	In stock	$ 165.00
25 mg	In stock	$ 275.00
50 mg	In stock	$ 397.00
100 mg	In stock	$ 593.00

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Purity: 99.1%

Purity: 98.73%

Purity: 98.34%

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Description	(Rac)-SAR131675 is an effective and specific VEGFR-3 inhibitor. It inhibited VEGFR-3 tyrosine kinase activity (IC50: 20 nmol/L) and VEGFR-3 autophosphorylation (IC50: 45 nmol/L) in HEK cells, respectively. SAR131675 is highly specific for VEGFR-3 versus 107 receptors, enzymes, ion channels, and 65 kinases. SAR131675 is a highly specific VEGFR-3-TK inhibitor with significant antitumoral and antimetastatic activities in vivo through inhibition of lymphangiogenesis and TAM invasion.
Targets&IC50	VEGFR3:20 nmol/L, VEGFR3:45 nmol/L
In vitro	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 nM. SAR131675 dose dependently inhibits rh-VEGFR-3–TK activity with an IC50 of 23 nM. SAR131675 inhibits VEGR-3–TK activity with a Ki of about 12 nM. SAR131675 inhibits VEGFR-1–TK activity with an IC50 of > 3 μM and VEGFR-2–TK activity with an IC50 of 235 nM. SAR131675 inhibits VEGFR-1 autophosphorylation with an IC50 of about 1 μM and VEGFR-2 with an IC50 of about 280 nM. SAR131675 moderately inhibits VEGFR-2 and has very little effect on VEGFR-1, showing a good selectivity for VEGFR-3. SAR131675 inhibits VEGFA-induced VEGFR-2 phosphorylation in a dose-dependent manner, with an IC50 of 239 nM. SAR131675 potently inhibits lymphatic cell survival induced by VEGFC and VEGFD with IC50 of 14 nM and 17 nM, respectively. SAR131675 inhibits VEGFA-induced survival with an IC50 of 664 nM. SAR131675, significantly and dose dependently inhibits VEGFC-induced Erk phosphorylation, with an IC50 of about 30 nM. [1]

Synonyms	SAR131675
Molecular Weight	358.39
Formula	C18H22N4O4
CAS No.	1092539-44-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: Slightly soluble

References and Literature

1. Alam A, et al. Mol Cancer Ther, 2012, 11(8), 1637-1649.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Kinase Inhibitor Library Anti-Cancer Active Compound Library Tyrosine Kinase Inhibitor Library Anti-Cardiovascular Disease Compound Library Reprogramming Compound Library Anti-Cancer Compound Library Cytokine Inhibitor Library Preclinical Compound Library Bioactive Compound Library

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Keywords

(Rac)-SAR131675 1092539-44-0 Angiogenesis Tyrosine Kinase/Adaptors VEGFR Vascular endothelial growth factor receptor potent (Rac)-SAR-131675 Inhibitor inhibit SAR-131675 (Rac) SAR131675 SAR131675 selective SAR 131675 racemate (Rac)SAR131675 inhibitor

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