AS703026 Inhibitor CAS No. 1236699-92-5

Cat. No.	Name	Size	Price
KI0637	AS703026	5 mg	$144
	AS703026	10 mg	$240
	AS703026	25 mg	$432
	AS703026	50 mg	$720

Chemical Characteristic

Product Name	AS703026
Synonyms	Pimasertib, MSC1936369
CAS No.	1236699-92-5
Molecular Weight	431.2
Formula	C₁₅H₁₅FIN₃O₃
Chemical Structure

Biological activities

AS703026 is a novel, selective, orally bioavailable mitogen-activated protein kinase (MEK) 1/2 inhibitor, in human multiple myeloma (MM). AS703026 inhibits growth of INA-6 and U266 cells with IC50 of 10 and 5 nM, respectively. AS703026 further induces apoptosis via caspase 3 and poly ADP-ribose polymerase (PARP) cleavage in MM cells, both in the presence or absence of bone marrow stromal cells (BMSCs). Treatment with AS703026 significantly diminishes basal levels of phosphorylated extracellular signal-regulated kinase (pERK) in U266 cells in a time- and dose-dependent fashion. AS703026 modulates the cell cycle in MM cells, increasing subG0 and decreasing S phase cell population in both H929 and U266 cells in a time-dependent manner.^[1] AS703026 inhibits human myeloma cell lines (HMCL) and cytokine-induced osteoclast differentiation, with an IC50 ranging from 0.005 to 2 µM. ^[2] AS703026 treatment significantly reduces the percentage of CD34⁺ cells and microvascular density in H929 tumors in vivo. ^[1]

Protocols

In vitro, AS703026 is dissolved in DMSO (10mM) and stored at -20°C. In vivo, AS703026 is suspended in 0.5% carboxymethylcellulose (CMC)/ 0.25% Tween 20 at 10 mg/mL. ^[1]

References

[1] Kim K, et al. 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, 149(4): 537-549. 閵嗏偓閵嗏偓 [2] Chang-Yew Leow C, et al. MEK inhibitors as a chemotherapeutic intervention in multiple myeloma. Blood Cancer J. 2013, 3: e105.

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