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.


Price and Availability

Size
Price

10mg
USD 90
100mg
USD 450
1g
USD 1950
Size
Price

25mg
USD 150
200mg
USD 750
2g
USD 2950
Size
Price

50mg
USD 250
500mg
USD 1250
5g
Ask price

VX-702, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide).


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 203162
Name: VX-702
CAS#: 745833-23-2 (or 479543-46-9)
Chemical Formula: C19H12F4N4O2
Exact Mass: 404.08964
Molecular Weight: 404.31779
Elemental Analysis: C, 56.44; H, 2.99; F, 18.80; N, 13.86; O, 7.91


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


Technical Data

Appearance:
White to off-white solid powder

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

Safety Data Sheet (MSDS):

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).

Harmonized System Code:
293490


Additional Information

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). 


References

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.