VX-702 | CAS#479543-46-9 | CAS#745833-23-2 | p38 MAP Kinase Inhibitor

VX-702
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 203162

CAS#: 745833-23-2 (or 479543-46-9)

Description: VX-702, one of a series of second-generation, is an orally active p38 MAP kinase inhibitors, for the potential treatment of inflammation, rheumatoid arthritis and cardiovascular diseases. VX-702 prevents activation of p38MAPK and decrements in many platelet storage parameters after exposure to 16 °C without agitation for 24 h.

Chemical Structure

VX-702

CAS# 745833-23-2 (or 479543-46-9)

Instruction

Theoretical Analysis

MedKoo Cat#: 203162
Name: VX-702
CAS#: 745833-23-2 (or 479543-46-9)
Chemical Formula: C19H12F4N4O2
Exact Mass: 404.09
Molecular Weight: 404.318
Elemental Analysis: C, 56.44; H, 2.99; F, 18.80; N, 13.86; O, 7.91

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 90
25mg	USD 150
50mg	USD 250
100mg	USD 450
200mg	USD 750
500mg	USD 1250
1g	USD 1950
2g	USD 2950
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: VX702, VX 702, VX-702

IUPAC/Chemical Name: 6-[(Aminocarbonyl)(2,6-difluorophenyl)amino]-2-(2,4-difluorophenyl)-3-pyridinecarboxamide

InChi Key: FYSRKRZDBHOFAY-UHFFFAOYSA-N

InChi Code: InChI=1S/C19H12F4N4O2/c20-9-4-5-10(14(23)8-9)16-11(18(24)28)6-7-15(26-16)27(19(25)29)17-12(21)2-1-3-13(17)22/h1-8H,(H2,24,28)(H2,25,29)

SMILES Code: O=C(C1=CC=C(N(C(N)=O)C2=C(F)C=CC=C2F)N=C1C3=CC=C(F)C=C3F)N

Appearance: White to off-white 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: >5 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: p38 MAPK increases thromboxane levels by activating phospholipase A2, thus catalyzing the formation of arachidonic acid. VX-702 inhibited activation of p38 MAPK by thrombin, SFLLRN, AYPGKF and U46619 in platelets. Kuliopulos, A., et al. "Effect of selective inhibition of the p38 MAP kinase pathway on platelet aggregation." Thromb. Haemost. 92: 1387-1393 (2004). VX-702 showed modest clinical efficacy and transient suppression of biomarkers of inflammation in patients with rheumatoid arthritis. Damjanov, N., et al. "Efficacy, pharmacodynamics, and safety of VX-702, a novel p38 MAPK inhibitor, in rheumatoid arthritis: results of two randomized, double-blind, placebo-controlled clinical studies." Arthritis Rheum. 60: 1232-1241 (2009).

Safety Data Sheet (SDS):

View Safety Data Sheet (SDS)

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 404.32 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.

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: Wagner SJ, Skripchenko A, Seetharaman S, Kurtz J. Amelioration of lesions associated with 24-hour suboptimal platelet storage at 16 °C by a p38MAPK inhibitor, VX-702. Vox Sang. 2015 Apr;108(3):226-32. doi: 10.1111/vox.12221. Epub 2014 Dec 4. PubMed PMID: 25471280.

2: Skripchenko A, Awatefe H, Thompson-Montgomery D, Myrup A, Turgeon A, Wagner SJ. An inhibition of p38 mitogen activated protein kinase delays the platelet storage lesion. PLoS One. 2013 Aug 13;8(8):e70732. doi: 10.1371/journal.pone.0070732. eCollection 2013. PubMed PMID: 23967093; PubMed Central PMCID: PMC3742641.

3: Tamhane M, Chakilam AR, Jayaraj A, Thakkar V, Taft DR. Comparative renal excretion of VX-702, a novel p38 MAPK inhibitor, and methotrexate in the perfused rat kidney model. Drug Dev Ind Pharm. 2010 Mar;36(3):315-22. doi: 10.3109/03639040903154200. PubMed PMID: 20170280.

4: Cohen S, Fleischmann R. Kinase inhibitors: a new approach to rheumatoid arthritis treatment. Curr Opin Rheumatol. 2010 May;22(3):330-5. doi: 10.1097/BOR.0b013e3283378e6f. Review. PubMed PMID: 20164774.

5: Goldstein DM, Kuglstatter A, Lou Y, Soth MJ. Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders. J Med Chem. 2010 Mar 25;53(6):2345-53. doi: 10.1021/jm9012906. PubMed PMID: 19950901.

6: Sweeney SE. The as-yet unfulfilled promise of p38 MAPK inhibitors. Nat Rev Rheumatol. 2009 Sep;5(9):475-7. doi: 10.1038/nrrheum.2009.171. PubMed PMID: 19710669.

7: Damjanov N, Kauffman RS, Spencer-Green GT. Efficacy, pharmacodynamics, and safety of VX-702, a novel p38 MAPK inhibitor, in rheumatoid arthritis: results of two randomized, double-blind, placebo-controlled clinical studies. Arthritis Rheum. 2009 May;60(5):1232-41. doi: 10.1002/art.24485. Erratum in: Arthritis Rheum. 2009 Oct;60(10):3071. PubMed PMID: 19404957.

8: Genovese MC. Inhibition of p38: has the fat lady sung? Arthritis Rheum. 2009 Feb;60(2):317-20. doi: 10.1002/art.24264. PubMed PMID: 19180514.

9: Ding C. Drug evaluation: VX-702, a MAP kinase inhibitor for rheumatoid arthritis and acute coronary syndrome. Curr Opin Investig Drugs. 2006 Nov;7(11):1020-5. PubMed PMID: 17117592.

10: Lee MR, Dominguez C. MAP kinase p38 inhibitors: clinical results and an intimate look at their interactions with p38alpha protein. Curr Med Chem. 2005;12(25):2979-94. Review. PubMed PMID: 16378500.

11: Dominguez C, Powers DA, Tamayo N. p38 MAP kinase inhibitors: many are made, but few are chosen. Curr Opin Drug Discov Devel. 2005 Jul;8(4):421-30. Review. PubMed PMID: 16022178.

12: Kuliopulos A, Mohanlal R, Covic L. Effect of selective inhibition of the p38 MAP kinase pathway on platelet aggregation. Thromb Haemost. 2004 Dec;92(6):1387-93. PubMed PMID: 15583748.

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