Pimasertib (AS-703026) - Moligand™, 10mM in DMSO , Dual specificity mitogen-activated protein kinase kinase 2 inhibitor, CAS No.1236699-92-5, Dual specificity mitogen-activated protein kinase kinase 2 inhibitor

CAS: 1236699-92-5 Cat. No.: P408137 Molecular Weight: 431.2

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

MSC1936369B, SAR 245509 | (S)-N-(2,3-dihydroxypropyl)-3-(2-fluoro-4-iodophenylamino)isonicotinamide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Pimasertib (AS-703026, MSC1936369B, SAR 245509) is a highly selective, potent, ATP non-competitive allosteric inhibitor ofMEK1/2withIC50of 5 nM-2 μM in MM cell lines. Phase 2.
In vitro

AS703026 is a novel, selective, orally bioavailable MEK1/2 inhibitor that binds to the distinctive MEK allosteric site and therefore exhibits exquisite kinase selectivity. AS703026 inhibits growth and survival of human multiple myeloma (MM) cells, including U266 and INA-6, with IC50 of 5 nM and 11 nM, respectively. Such an inhibitory effect by AS703026 is mediated by G0-G1 cell cycle arrest and is accompanied by reduced expresson of the MAF oncogene. AS703026 further induces apoptosis via caspase-3 and PARP cleavage in MM cells, both in the presence or absence of bone marrow stromal cells (BMSCs). AS703026 may be an effective therapy in colorectal cancer caused by K-Ras mutation. AS703026 (10 μM) effectively inhibits the ERK pathway, proliferation, and transformation in human DLD-1 colorectal cancer cells what carry a mutant allele of K-Ras (D-MUT).

In vivo

AS703026 (15 and 30 mg/kg) significantly inhibits tumor growth in a human plasmacytoma xenograft model of H929 MM cells. This can be correlated with downregulated pERK1/2, induced PARP cleavage, and decreased microvessels. AS703026 (10 mg/kg) inhibits tumor growth, and markedly decreases p-ERK level in a xenograft mouse model of human K-Ras mutated (D-MUT) colorectal tumor.
Cell Data

cell lines：

Concentrations：2 nM - 20 μM (stock: 10 mM in DMSO)

Incubation Time：48 hours

Powder Purity:≥97%

Specifications

Synonyms

MSC1936369B, SAR 245509 | (S)-N-(2, 3-dihydroxypropyl)-3-(2-fluoro-4-iodophenylamino)isonicotinamide

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Pimasertib (AS-703026, MSC1936369B, SAR 245509) is a highly selective, potent, ATP non-competitive allosteric inhibitor of MEK1/2 with IC50 of 5 nM-2 μM in MM cell lines. Phase 2.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

Dual specificity mitogen-activated protein kinase kinase 2 inhibitor

Names and Identifiers

• Isomeric SMILES: C1=CC(=C(C=C1I)F)NC2=C(C=CN=C2)C(=O)NC[C@@H](CO)O
• Molecular Weight: 431.2
• Reaxy-Rn: 40713281
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=40713281&ln=

Associated Targets(Human)

IARS2 Tchem Isoleucine--tRNA ligase, mitochondrial (1 Activities)

Discover Target: IARS2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MAP2K1 Tclin Dual specificity mitogen-activated protein kinase kinase 1 (3 Activities)

Discover Target: MAP2K1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro DMSO: 48 mg/mL (196.52 mM); Ethanol: 48 mg/mL (196.52 mM); Water: Insoluble