AS703026
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- Product name: AS703026
- CAS: 1236699-92-5
- MF: C15H15FIN3O3
- MW: 431.2
- EINECS:
- MDL Number:MFCD16660676
- Synonyms:AS703026;N-[(2S)-2,3-Dihydroxypropyl]-3-[(2-fluoro-4-iodophenyl)amino]-4-pyridinecarboxamide;(S)-N-(2,3-dihydroxypropyl)-3-(2-fluoro-4-iodophenylaMino)isonicotinaMide;4-PyridinecarboxaMide, N-[(2S)-2,3-dihydroxypropyl]-3-[(2-fluoro-4-iodophenyl)aMino]-;MSC1936369B;PiMasertib (AS-703026);AS703026/MSC1936369B;PiMasertib
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Properties
Boiling point :623.2±55.0 °C(Predicted)
Density :1.769
storage temp. :Store at -20°C
solubility :≥21.55 mg/mL in DMSO; insoluble in H2O; ≥10.36 mg/mL in EtOH with ultrasonic
form :solid
pka :12.82±0.46(Predicted)
color :Light yellow to khaki
Density :1.769
storage temp. :Store at -20°C
solubility :≥21.55 mg/mL in DMSO; insoluble in H2O; ≥10.36 mg/mL in EtOH with ultrasonic
form :solid
pka :12.82±0.46(Predicted)
color :Light yellow to khaki
Safety Information
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Description
The mitogen-activated protein kinases, MEK1 and 2, are dual-specificity threonine/tyrosine kinases that play key roles in the activation of the Ras-Raf-MEK-ERK pathway and are often upregulated in a variety of cancer cell types. AS-703026 is an orally bioavailable small molecule that selectively binds to and inhibits MEK1/2, preventing the activation of downstream effector proteins and transcription factors. It potently inhibits growth and survival of human INA-6 multiple myeloma cells and cytokine-induced osteoclast differentiation with IC50 values of 10 and 18.2 nM, respectively. In mice bearing H929 MM xenograft tumors, 30 mg/kg AS-703026 reduced tumor growth significantly, which correlated with downregulated ERK1/2 activity, induced PARP cleavage, and decreased microvessels in vivo. At 10 μM, AS-703026 supressed proliferation and transformation of K-Ras mutated colorectal cancer cells resistant to EGFR antibody therapy.Related product price
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