AMG-47a - CAS 882663-88-9
Catalog number: 882663-88-9
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C29H28F3N5O2
Molecular Weight:
535.56
COA:
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Targets:
Src
Description:
AMG-47a is a potent inhibitor of Lck and T cell proliferation. It has anti-inflammatory activity (ED50 = 11 mg/kg) in the anti-CD3 induced production of IL-2 in mice. It displays subnanomolar inhibition against Lck, and low inhibition against other hard to inhibit kinases in several other in vitro assays. It effectively inhibits the JNK family of kinases including TYK2 at ~ 1.2 μM but well under 10 μM. It selectively reduced the levels of EGFP-KRASG12V protein but did not affect EGFP protein in cells.
Purity:
95%
Appearance:
Solid powder
Synonyms:
4-Methyl-3-[2-[[2-(4-morpholinyl)ethyl]amino]-6-quinazolinyl]-N-[3-(trifluoromethyl)phenyl]benzamide
Solubility:
10 mM in DMSO
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
AMG-47a has anti-inflammatory activity.
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Grams to Kilograms
Density:
1.324±0.06 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr
InChIKey:
DVRSTRMZTAPMKO-UHFFFAOYSA-N
InChI:
InChI=1S/C29H28F3N5O2/c1-19-5-6-21(27(38)35-24-4-2-3-23(17-24)29(30,31)32)16-25(19)20-7-8-26-22(15-20)18-34-28(36-26)33-9-10-37-11-13-39-14-12-37/h2-8,15-18H,9-14H2,1H3,(H,35,38)(H,33,34,36)
Canonical SMILES:
CC1=C(C=C(C=C1)C(=O)NC2=CC=CC(=C2)C(F)(F)F)C3=CC4=CN=C(N=C4C=C3)NCCN5CCOCC5
1.A high-throughput assay for small molecule destabilizers of the KRAS oncoprotein.
Carver J;Dexheimer TS;Hsu D;Weng MT;Smith JL;Guha R;Jadhav A;Simeonov A;Luo J PLoS One. 2014 Aug 5;9(8):e103836. doi: 10.1371/journal.pone.0103836. eCollection 2014.
Mutations in the Ras family of small GTPases, particularly KRAS, occur at high frequencies in cancer and represent a major unmet therapeutic need due to the lack of effective targeted therapies. Past efforts directed at inhibiting the activity of the Ras oncoprotein have proved difficult. We propose an alternative approach to target Ras by eliminating Ras protein from cells with pharmacological means. In this study, we developed a cell-based, high-content screening platform to identify small molecules that could promote the degradation of the KRAS oncoprotein. We generated an EGFP-KRASG12V fluorescence reporter system and implemented it for automated screening in 1536-well plates using high-throughput cellular imaging. We screened a library of clinically relevant compounds at wide dose range and identified Ponatinib and AMG-47a as two candidate compounds that selectively reduced the levels of EGFP-KRASG12V protein but did not affect EGFP protein in cells. This proof-of-principle study demonstrates that it is feasible to use a high-throughput screen to identify compounds that promote the degradation of the Ras oncoprotein as a new approach to target Ras.
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CAS 882663-88-9 AMG-47a

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