Chemical Structure : BIM-46174
CAS No.:
195450-11-4
BIM-46174
(BIM46174)
Catalog No.: PC-23379Not For Human Use, Lab Use Only.
BIM-46174 is a selective inhibitor of heterotrimeric G-protein complex Gα/Gβγ subunits, abrogates cancer cell invasion controlled by several GPCR agonists.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
BIM-46174 is a selective inhibitor of heterotrimeric G-protein complex Gα/Gβγ subunits, abrogates cancer cell invasion controlled by several GPCR agonists.
BIM-46174 competitively inhibitscholera toxin–induced cAMP accumulation with a pA2 value of 5.3.
BIM-46174 only affects cAMP generation induced by cholera toxin via Gαs and not by forskolin directly acting on adenylyl cyclase. BIM46174 has no effect on cancer cell invasion induced by individual subunits of heterotrimeric G-protein complex: Gα12, Gα13, or Gβ1γ2 dimer.
BIM46174 inhibits the growth of a large panel of human cancer cell lines, including anticancer drug-resistant cells.
BIM-46174 combined with either cisplatin, farnesyltransferase inhibitor, or topoisomerase inhibitors, significantly reduced the growth rate of human tumor xenografts in athymic mice.
Physicochemical Properties
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M.Wt
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398.57
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Formula
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C22H30N4OS
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(R)-2-amino-1-((S)-8-(cyclohexylmethyl)-2-phenyl-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl)-3-mercaptopropan-1-one
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References
1. Prévost GP, et al. Cancer Res. 2006 Sep 15;66(18):9227-34.
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