SAR131675

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 407300

CAS#: 1092539-44-0

Description: SAR131675 is a potent and selective VEGFR-3 inhibitor. It inhibited VEGFR-3 tyrosine kinase activity and VEGFR-3 autophosphorylation in HEK cells with IC(50) values of 20 and 45 nmol/L, respectively. SAR131675 was found to be highly selective for VEGFR-3 versus 107 receptors, enzymes, ion channels, and 65 kinases. SAR131675 is the first highly specific VEGFR-3-TK inhibitor described to date, displaying significant antitumoral and antimetastatic activities in vivo through inhibition of lymphangiogenesis and TAM invasion.


Chemical Structure

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SAR131675
CAS# 1092539-44-0

Theoretical Analysis

MedKoo Cat#: 407300
Name: SAR131675
CAS#: 1092539-44-0
Chemical Formula: C18H22N4O4
Exact Mass: 358.16
Molecular Weight: 358.398
Elemental Analysis: C, 60.32; H, 6.19; N, 15.63; O, 17.86

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Related CAS #: 1433953-83-3   1092538-80-1  

Synonym: SAR131675; SAR 131675; SAR-131675.

IUPAC/Chemical Name: 2-amino-1-ethyl-7-(3-hydroxy-4-methoxy-3-methylbut-1-yn-1-yl)-N-methyl-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxamide

InChi Key: PFMPOBVAYMTUOX-UHFFFAOYSA-N

InChi Code: InChI=1S/C18H22N4O4/c1-5-22-15(19)13(17(24)20-3)14(23)12-7-6-11(21-16(12)22)8-9-18(2,25)10-26-4/h6-7,25H,5,10,19H2,1-4H3,(H,20,24)

SMILES Code: O=C(C(C(NC)=O)=C(N)N1CC)C2=C1N=C(C#CC(O)(COC)C)C=C2

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 358.40 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Yu J, Mao L, Guan L, Zhang Y, Zhao J. Ginsenoside Rg1 enhances lymphatic transport of intrapulmonary silica via VEGF-C/VEGFR-3 signaling in silicotic rats. Biochem Biophys Res Commun. 2016 Mar 25;472(1):182-8. doi: 10.1016/j.bbrc.2016.02.091. Epub 2016 Feb 23. PubMed PMID: 26920056.

2: Bhuiyan MI, Kim JC, Hwang SN, Lee MY, Kim SY. Ischemic tolerance is associated with VEGF-C and VEGFR-3 signaling in the mouse hippocampus. Neuroscience. 2015 Apr 2;290:90-102. doi: 10.1016/j.neuroscience.2015.01.025. Epub 2015 Jan 28. PubMed PMID: 25637798.

3: Nihei M, Okazaki T, Ebihara S, Kobayashi M, Niu K, Gui P, Tamai T, Nukiwa T, Yamaya M, Kikuchi T, Nagatomi R, Ebihara T, Ichinose M. Chronic inflammation, lymphangiogenesis, and effect of an anti-VEGFR therapy in a mouse model and in human patients with aspiration pneumonia. J Pathol. 2015 Mar;235(4):632-45. doi: 10.1002/path.4473. Epub 2015 Jan 7. PubMed PMID: 25348279.

4: Osborn AJ, Dickie P, Neilson DE, Glaser K, Lynch KA, Gupta A, Dickie BH. Activating PIK3CA alleles and lymphangiogenic phenotype of lymphatic endothelial cells isolated from lymphatic malformations. Hum Mol Genet. 2015 Feb 15;24(4):926-38. doi: 10.1093/hmg/ddu505. Epub 2014 Oct 6. PubMed PMID: 25292196.

5: Espagnolle N, Barron P, Mandron M, Blanc I, Bonnin J, Agnel M, Kerbelec E, Herault JP, Savi P, Bono F, Alam A. Specific Inhibition of the VEGFR-3 Tyrosine Kinase by SAR131675 Reduces Peripheral and Tumor Associated Immunosuppressive Myeloid Cells. Cancers (Basel). 2014 Feb 28;6(1):472-90. doi: 10.3390/cancers6010472. PubMed PMID: 24589997; PubMed Central PMCID: PMC3980599.

6: Alam A, Blanc I, Gueguen-Dorbes G, Duclos O, Bonnin J, Barron P, Laplace MC, Morin G, Gaujarengues F, Dol F, Hérault JP, Schaeffer P, Savi P, Bono F. SAR131675, a potent and selective VEGFR-3-TK inhibitor with antilymphangiogenic, antitumoral, and antimetastatic activities. Mol Cancer Ther. 2012 Aug;11(8):1637-49. doi: 10.1158/1535-7163.MCT-11-0866-T. Epub 2012 May 14. PubMed PMID: 22584122.