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Cat. No. M1652
AS703026 Structure


Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM/1mL In DMSO USD 60 In stock
10mg USD 70 In stock
50mg USD 180 In stock
200mg USD 480 In stock
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Quality Control
Biological Activity

AS703026 is a novel selective MEK1/2 inhibitor, induces pleiotropic anti-myeloma activity in vitro and in vivo. AS703026 inhibited growth and survival of MM cells and cytokine-induced osteoclast differentiation more potently (9- to 10-fold) than AZD6244. AS703026 further induced 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).

Customer Product Validations & Biological Datas
Source PLoS One (2015). Figure 2. AS-703026
Method trypan blue staining
Cell Lines RAW 264.7 cells
Concentrations 10–250 nM
Incubation Time 24 h
Results The activity of AS-703026 was dose-dependent, and was most significant at 250 nM
Source PLoS One (2015). Figure 1. AS-703026
Method MTT assay
Cell Lines RAW 264.7 cells
Concentrations 10–250 nM
Incubation Time 24 h
Results Significantly, AS-703026 at 10–250 nM dose-dependently inhibited LPS (100 ng/mL)-induced TNFα production in RAW 264.7 cells. Further, TNFα mRNA expression by the LPS treatment was also inhibited
Cell Experiment
Cell lines MM cell lines
Preparation method Cytotoxicity assays.
The inhibitory effects of study compounds on MM cell growth and survival were assessed by both [3H]thymidine incorporation and by measuring 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrasodium bromide (MTT; Sigma-Aldrich, St Louis, MO) dye absorbance following the manufacturer's instruction. Cells (104/well for MM cell line, in triplicates and 2-5×105/well for patient MM cells) were cultured in 96-well plates for 3 days (MM cell lines) or 5-days (patient MM cells). For the [3H]thymidine incorporation assay, cells were pulsed with 0.5 μCi (0.0185 MBq)/well [3H]thymidine (Amersham, Pittsburgh, PA) for 6 h (cell lines), harvested onto glass fiber filters, and counted in a β-scintillation counter. Due to low DNA synthesis of patient MM cells, they were pulsed with 2 μCi/well [3H]thymidine and measured during the last 36 h of culture.
Concentrations 0, 2, 20, 200, 2000, 20000 nM
Incubation time 3 days
Animal Experiment
Animal models H929 cells human plasmacytoma xenograft model
Formulation suspended in 0.5% carboxymethylcellulose (CMC)/0.25%Tween20 at 10 mg/ml
Dosages 15 or 30 mg/kg twice daily
Administration orally
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 431.20
Formula C15H15FIN3O3
CAS Number 1236699-92-5
Purity >99%
Solubility DMSO
Storage at -20°C

MEK1/2 inhibitors AS703026 and AZD6244 may be potential therapies for KRAS mutated colorectal cancer that is resistant to EGFR monoclonal antibody therapy.
Yoon et al. Cancer Res. 2011 Jan 15;71(2):445-53. PMID: 21118963.

Blockade of the MEK/ERK signaling cascade by AS703026, a novel selective MEK1/2 inhibitor, induces pleiotropic anti-myeloma activity in vitro and in vivo.
Kihyun et al. Br J Haematol. 2010 May;149(4): 537–549. PMID: 20331454.

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Keywords: AS703026, MSC1936369B,Pimasertib supplier, MEK, inhibitors

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