Pimasertib

• CAT Number: I000947
• CAS Number: 1236699-92-5
• Molecular Formula: C₁₅H₁₅FIN₃O₃
• Molecular Weight: 431.2
• Purity: ≥95%
• Synonyms: N-[(2S)-2,3-dihydroxypropyl]-3-(2-fluoro-4-iodoanilino)pyridine-4-carboxamide
• Target: MEK1/2
• Solubility: DMSO ≥83mg/mL Water <1.2mg/mL Ethanol ≥2.6mg/mL
• Storage: 3 years -20C powder
• InChI: 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
• InChIKey: VIUAUNHCRHHYNE-JTQLQIEISA-N
• SMILES: C1=CC(=C(C=C1I)F)NC2=C(C=CN=C2)C(=O)NCC(CO)O

Pimasertib, also known as AS703026 (CAT: I000947), is a selective inhibitor of MEK1 and MEK2, which are kinases involved in the MAPK/ERK signaling pathway. By inhibiting MEK1/2, pimasertib blocks the activation of downstream kinases, including ERK1/2. This pathway plays a crucial role in cell proliferation, survival, and differentiation. Pimasertib has shown potential as an anticancer agent, particularly in the treatment of melanoma. It interferes with the aberrant MAPK/ERK signaling that is often dysregulated in cancer cells, leading to reduced tumor growth and proliferation. Pimasertib represents a promising targeted therapy for certain types of cancers that rely on MAPK/ERK pathway activation.

Reference

1:Comprehensive Two- and Three-Dimensional RNAi Screening Identifies PI3K Inhibition as a Complement to MEK Inhibitor AS703026 for Combination Treatment of Triple-Negative Breast Cancer. Lee J, Galloway R, Grandjean G, Jacob J, Humphries J, Bartholomeusz C, Goodstal S, Lim B, Bartholomeusz G, Ueno NT, Rao A.J Cancer. 2015 Oct 28;6(12):1306-19. doi: 10.7150/jca.13266. eCollection 2015. PMID: 26640591 Free PMC Article2:The MEK1/2 inhibitor AS703026 circumvents resistance to the BRAF inhibitor PLX4032 in human malignant melanoma cells. Park SJ, Hong SW, Moon JH, Jin DH, Kim JS, Lee CK, Kim KP, Hong YS, Choi EK, Lee JS, Lee JL, Kim TW.Am J Med Sci. 2013 Dec;346(6):494-8. doi: 10.1097/MAJ.0b013e318298a185. PMID: 24051957 3:MEK1/2 inhibitors AS703026 and AZD6244 may be potential therapies for KRAS mutated colorectal cancer that is resistant to EGFR monoclonal antibody therapy. Yoon J, Koo KH, Choi KY.Cancer Res. 2011 Jan 15;71(2):445-53. doi: 10.1158/0008-5472.CAN-10-3058. Epub 2010 Nov 30. PMID: 21118963 Free Article4: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. 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.Br J Haematol. 2010 May;149(4):537-49. doi: 10.1111/j.1365-2141.2010.08127.x. Epub 2010 Mar 12. PMID: 20331454 Free PMC Article