AS-703026
Product Code:
SYN-1190
SYN-1190
Regulatory Status:
RUO
RUO
Shipping:
4°C
4°C
No additional charges, what you see is what you pay! *
Code | Size | Price |
---|
SYN-1190-M100 | 100 mg | Enquire |
Quantity:
SYN-1190-M001 | 1 mg | £80.00 |
Quantity:
SYN-1190-M005 | 5 mg | £115.00 |
Quantity:
SYN-1190-M010 | 10 mg | £151.00 |
Quantity:
SYN-1190-M050 | 50 mg | £467.00 |
Quantity:
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This product comes from: Switzerland.
Typical lead time: 7-10 working days.
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Typical lead time: 7-10 working days.
Contact us for more accurate information.
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Further Information
Alternate Names/Synonyms:
AS703026
Appearance:
Solid.
CAS:
1236699-92-5
EClass:
32160000
Form (Short):
liquid
InChi:
InChI=1S/C15H15FIN3O3/c16-12-5-9(17)1-2-13(12)20-14-7-18-4-3-11(14)15(23)19-6-10(22)8-21/h1-5,7,10,20-22H,6,8H2,(H,19,23)/t10-/m0/s1
InChiKey:
VIUAUNHCRHHYNE-JTQLQIEISA-N
Long Description:
Chemical. CAS: 1236699-92-5. Formula: C15H15FIN3O3. MW: 431.2. AS703026 is a novel, selective, non-competitive, orally bioavailable MEK1/2 inhibitor with experimental IC(50) values of 5-11nM. In use on multiple myeloma cells (MM), AS703026 inhibited growth and survival of MM cells and cytokine-induced osteoclast differentiation more potently (~10X) than AZD6244. Inhibition of proliferation induced by AS703026 was mediated by G0-G1 cell cycle arrest and was accompanied by reduction of MAF oncogene expression. 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). Importantly, AS703026 sensitized MM cells to a broad spectrum of conventional (dexamethasone, melphalan), novel or emerging (lenalidomide, perifosine, bortezomib, rapamycin) anti-MM therapies. Significant tumour growth reduction in AS703026- vs. vehicle-treated mice bearing H929 MM xenograft tumours correlated with downregulated pERK1/2, induced PARP cleavage, and decreased microvessels in vivo. Moreover, AS703026 (<200nM) was cytotoxic against the majority of tumour cells tested from patients with relapsed and refractory MM (84%), regardless of mutational status of RAS and BRAF genes. Importantly, BMSC-induced viability of MM patient cells was similarly blocked within the same dose range.
Molecular Formula:
C15H15FIN3O3
Molecular Weight:
431.2
Package Type:
Plastic Vial
Product Description:
AS703026 is a novel, selective, non-competitive, orally bioavailable MEK1/2 inhibitor with experimental IC(50) values of 5-11nM. In use on multiple myeloma cells (MM), AS703026 inhibited growth and survival of MM cells and cytokine-induced osteoclast differentiation more potently (~10X) than AZD6244. Inhibition of proliferation induced by AS703026 was mediated by G0-G1 cell cycle arrest and was accompanied by reduction of MAF oncogene expression. 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). Importantly, AS703026 sensitized MM cells to a broad spectrum of conventional (dexamethasone, melphalan), novel or emerging (lenalidomide, perifosine, bortezomib, rapamycin) anti-MM therapies. Significant tumour growth reduction in AS703026- vs. vehicle-treated mice bearing H929 MM xenograft tumours correlated with downregulated pERK1/2, induced PARP cleavage, and decreased microvessels in vivo. Moreover, AS703026 (< 200nM) was cytotoxic against the majority of tumour cells tested from patients with relapsed and refractory MM (84%), regardless of mutational status of RAS and BRAF genes. Importantly, BMSC-induced viability of MM patient cells was similarly blocked within the same dose range.
Purity:
>95%
Solubility Chemicals:
Soluble in DMSO. Slightly soluble (<1mg/ml) in ethanol.
Transportation:
Non-hazardous
UNSPSC Category:
Protein Kinase Modulators
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 1 year after receipt when stored at +4°C.
Documents
References
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: K. Kim, et al.; Br. J. Haematol. 149, 537 (2010) | MEK1/2 inhibitors AS703026 and AZD6244 may be potential therapies for KRAS mutated colorectal cancer that is resistant to EGFR monoclonal antibody therapy: J. Yoon, et al.; J. Cancer Res. 71, 445 (2011)