1. MAPK/ERK Pathway
  2. MEK

AS703026 (Synonyms: Pimasertib; MSC1936369B; AS-703026; AS 703026)

Cat. No.: HY-12042
Handling Instructions

AS703026(Pimasertib) is a highly selective, potent, ATP non-competitive allosteric inhibitor of MEK1/2 with IC50 of 5 nM-2 μM in MM cell lines.

For research use only. We do not sell to patients.
AS703026 Chemical Structure

AS703026 Chemical Structure

CAS No. : 1236699-92-5

Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO $55 In-stock
5 mg $50 In-stock
10 mg $70 In-stock
50 mg $180 In-stock
100 mg $270 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Description

AS703026(Pimasertib) is a highly selective, potent, ATP non-competitive allosteric inhibitor of MEK1/2 with IC50 of 5 nM-2 μM in MM cell lines. IC50 value: Target: MEK1/2 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). [1] 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). [2] 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. [1] 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. [2]

Clinical Trial
Sponsor Condition Start Date Phase
EMD Serono Inc Peritoneal tumor 2013-09-30 Phase 2
EMD Serono Inc Ovary tumor 2013-09-30 Phase 2
EMD Serono Inc Melanoma 2012-11-30 Phase 2
EMD Serono Inc Metastatic colorectal cancer 2010-03-31 Phase 2
EMD Serono Inc Pancreas tumor 2009-11-30 Phase 2
EMD Serono Inc Adenocarcinoma 2009-11-30 Phase 2
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 2.3191 mL 11.5955 mL 23.1911 mL
5 mM 0.4638 mL 2.3191 mL 4.6382 mL
10 mM 0.2319 mL 1.1596 mL 2.3191 mL
M.Wt

431.2

Formula

C₁₅H₁₅FIN₃O₃

CAS No.

1236699-92-5

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

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AS703026
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HY-12042
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