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Signaling Pathway

AS703026

HY-12042

(Pimasertib; MSC1936369B; AS-703026; AS 703026)

AS703026

AS703026 Chemical Structure

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.

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Free sample   Apply now  
10 mM * 1 mL in DMSO $55 In-stock
5 mg $50 In-stock
10 mg $65 In-stock
50 mg $180 In-stock
100 mg $287 In-stock
200 mg Get quote
500 mg Get quote
Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO €54 In-stock
5 mg €49 In-stock
10 mg €64 In-stock
50 mg €176 In-stock
100 mg €281 In-stock
200 mg Get quote
500 mg Get quote

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Product name: AS703026
Cat. No.: HY-12042

AS703026 Data Sheet

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    Purity: 99.95%

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Related Compound Libraries

Biological Activity of AS703026

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]

Chemical Information

M.Wt 431.2 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C15H15FIN3O3
CAS No 1236699-92-5
Solvent & Solubility

DMSO ≥83mg/mL Water <1.2mg/mL Ethanol ≥2.6mg/mL

Preparing Stock Solutions

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

Clinical Information of AS703026

Product Name Sponsor Only Condition Start Date End Date Phase Last Change Date
AS703026 EMD Serono Inc Peritoneal tumor 30-SEP-13 31-MAR-16 Phase 2 13-SEP-13
EMD Serono Inc Ovary tumor 30-SEP-13 31-MAR-16 Phase 2 13-SEP-13
EMD Serono Inc Pancreas tumor 30-NOV-09 31-AUG-15 Phase 2 20-JUN-13
EMD Serono Inc Melanoma 30-NOV-12 31-OCT-14 Phase 2 27-MAR-13
EMD Serono Inc Adenocarcinoma 30-NOV-09 31-AUG-15 Phase 2 20-JUN-13
EMD Serono Inc Metastatic colorectal cancer 31-MAR-10 31-MAY-13 Phase 2 23-OCT-13

References on AS703026

Inhibitor Kit

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