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AS703026

Cat. No. M1652
AS703026 Structure
Synonym:

MSC1936369B,Pimasertib

Size Price Availability Quantity
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).

Protocol
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
References

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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  Catalog
Abmole Inhibitor Catalog 2017




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

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