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MedKoo Cat#: 414955 | Name: Pimasertib HCl

Description:

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

Pimasertib (AS703026, SAR245509, MSC1936369B) is a selective, orally bioavailable inhibitor of MEK1/2 (mitogen-activated protein kinase kinase 1/2), key components of the MAPK/ERK signaling pathway implicated in various cancers. It exhibits potent inhibitory activity with an IC₅₀ of ~5 nM for MEK1 and ~6 nM for MEK2 in enzymatic assays. In cellular models, Pimasertib effectively suppresses ERK1/2 phosphorylation with sub-nanomolar to low nanomolar IC₅₀ values in BRAF- or RAS-mutant tumor cell lines. It has shown antiproliferative effects across multiple tumor types, particularly melanoma, colorectal, and pancreatic cancers, often inducing apoptosis or cell cycle arrest.

Chemical Structure

Pimasertib HCl
Pimasertib HCl
CAS#1236361-78-6 (HCl)

Theoretical Analysis

MedKoo Cat#: 414955

Name: Pimasertib HCl

CAS#: 1236361-78-6 (HCl)

Chemical Formula: C15H16ClFIN3O3

Exact Mass: 0.0000

Molecular Weight: 467.66

Elemental Analysis: C, 38.52; H, 3.45; Cl, 7.58; F, 4.06; I, 27.14; N, 8.99; O, 10.26

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
1236699-92-5 (free base) 1236361-78-6 (HCl)
Synonym
Pimasertib hydrochloride; Pimasertib HCl; SAR245509; SAR-245509; SAR 245509; AS703026; AS 703026; AS-703026; MSC1936369B; MSC 1936369B; MSC-1936369B; Pimasertib;
IUPAC/Chemical Name
4-Pyridinecarboxamide, N-((2S)-2,3-dihydroxypropyl)-3-((2-fluoro-4-iodophenyl)amino)-, hydrochloride (1:1)
InChi Key
HIEXZUXKTABHCP-PPHPATTJSA-N
InChi Code
InChI=1S/C15H15FIN3O3.ClH/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);1H/t10-;/m0./s1
SMILES Code
O=C(C1=C(NC2=CC=C(I)C=C2F)C=NC=C1)NC[C@H](O)CO.[H]Cl
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
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
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

Preparing Stock Solutions

The following data is based on the product molecular weight 467.66 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.

Recalculate based on batch purity %
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.