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

MedKoo CAT#: 200297

CAS#: 1236699-92-5

Description: Pimasertib, also known as AS703026, SAR245509, MSC1936369B, is a n orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity. MEK inhibitor AS703026 selectively binds to and inhibits the activity of MEK1/2, preventing the activation of MEK1/2-dependent effector proteins and transcription factors, which may result in the inhibition of growth factor-mediated cell signaling and tumor cell proliferation.


Price and Availability

Size
Price

5mg
USD 165
Size
Price

10mg
USD 250
Size
Price

25mg
USD 450

Pimasertib ( AS-703026), 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.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 200297
Name: Pimasertib
CAS#: 1236699-92-5
Chemical Formula: C15H15FIN3O3
Exact Mass: 431.01421
Molecular Weight: 431.2
Elemental Analysis: C, 41.78; H, 3.51; F, 4.41; I, 29.43; N, 9.74; O, 11.13


Synonym: SAR245509; SAR245509; SAR 245509; MSC1936369B; AS703026; AS 703026; AS703026. Pimasertib

IUPAC/Chemical Name: (S)-N-(2,3-dihydroxypropyl)-3-((2-fluoro-4-iodophenyl)amino)isonicotinamide.

InChi Key: VIUAUNHCRHHYNE-JTQLQIEISA-N

InChi Code: InChI=1S/C15H15FIN3O3/c16-12-5-9(17)1-2-13(12)20-14-7-18-4-3-11(14)15(23)19-6-10(22)8-21/h1-5,7,10,20-22H,6,8H2,(H,19,23)/t10-/m0/s1

SMILES Code: O=C(NC[C@H](O)CO)C1=CC=NC=C1NC2=CC=C(I)C=C2F


Technical Data

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).

Harmonized System Code:
293490


Additional Information

 Related CAS#
1236699-92-5 (Pimasertib)
1236361-78-6 (Pimasertib Hydrochloride)
 


References

1: Zhang Y, Xue D, Wang X, Lu M, Gao B, Qiao X. Screening of kinase inhibitors targeting BRAF for regulating autophagy based on kinase pathways. Mol Med Rep. 2014 Jan;9(1):83-90. doi: 10.3892/mmr.2013.1781. Epub 2013 Nov 7. PubMed PMID: 24213221.

2: Park SJ, Hong SW, Moon JH, Jin DH, Kim JS, Lee CK, Kim KP, Hong YS, Choi EK, Lee JS, Lee JL, Kim TW. The MEK1/2 inhibitor AS703026 circumvents resistance to the BRAF inhibitor PLX4032 in human malignant melanoma cells. Am J Med Sci. 2013 Dec;346(6):494-8. doi: 10.1097/MAJ.0b013e318298a185. PubMed PMID: 24051957.

3: Sarris EG, Syrigos KN, Saif MW. Novel agents and future prospects in the treatment of pancreatic adenocarcinoma. JOP. 2013 Jul 10;14(4):395-400. doi: 10.6092/1590-8577/1654. PubMed PMID: 23846936.

4: Yoon J, Koo KH, Choi KY. MEK1/2 inhibitors AS703026 and AZD6244 may be potential therapies for KRAS mutated colorectal cancer that is resistant to EGFR monoclonal antibody therapy. Cancer Res. 2011 Jan 15;71(2):445-53. doi: 10.1158/0008-5472.CAN-10-3058. Epub 2010 Nov 30. PubMed PMID: 21118963.

5: Kim K, Kong SY, Fulciniti M, Li X, Song W, Nahar S, Burger P, Rumizen MJ, Podar K, Chauhan D, Hideshima T, Munshi NC, Richardson P, Clark A, Ogden J, Goutopoulos A, Rastelli L, Anderson KC, Tai YT. Blockade of the MEK/ERK signalling cascade by AS703026, a novel selective MEK1/2 inhibitor, induces pleiotropic anti-myeloma activity in vitro and in vivo. Br J Haematol. 2010 May;149(4):537-49. doi: 10.1111/j.1365-2141.2010.08127.x. Epub 2010 Mar 12. PubMed PMID: 20331454; PubMed Central PMCID: PMC3418597.