WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 200297
CAS#: 1236699-92-5 (free base)
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.
MedKoo Cat#: 200297
CAS#: 1236699-92-5 (free base)
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
Related CAS #: 1236361-78-6 (HCl); 1236699-92-5 (free base)
Synonym: SAR245509; SAR-245509; SAR 245509; MSC1936369B; AS703026; AS 703026; AS-703026; 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
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
The following data is based on the product molecular weight 431.2 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|
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.
1236361-78-6 (Pimasertib Hydrochloride)