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CAS No. : 2070014-99-0
MCE 国际站:GNE-617 hydrochloride
产品活性:GNE-617 hydrochloride 是一种特异性的 NAMPT 抑制剂,抑制 NAMPT 活性,IC50 为 5 nM。
研究领域:Metabolic Enzyme/Protease
作用靶点:NAMPT
In Vitro: The activity ofGNE-617 hydrochloride is evaluated on a panel 53 non-small cell lung cancer (NSCLC) cell lines in the presence or absence of 10 μM nicotinic acid. GNE-617 inhibits NAMPT IC50 of 18.9 nM in A549 cell.The majority of cell lines exhibit a steep dose response to GNE-617 when evaluated by decrease in ATP or total nucleic acid, and the cytotoxicity is completely rescued by simultaneous addition of nicotinic acid. The majority of the cell lines tested have IC50 values below 100 nM, with approximately half with IC50 values less than 10 nM. Eighteen cell lines are not rescued with nicotinic acid, and these non-rescuable cell lines tended to have lower IC50 values (P=0.008, Fisher exact test, IC50<10 nM vs. ≥10 nM).
In Vivo: In rats, GNE-617 hydrochloride (administered QD) and GNE-875 (administered BID) are associated with more severe retinal toxicity at similar exposures and dosing duration compared with GMX-1778 (administered BID). The mouse efficacy studies using GNE-617, GNE-618, and GMX-1778 are designed to assess efficacy and opportunistically used to assess retinal toxicity in mice. NAMPTi retinal toxicity is observed with GNE-617 and GMX-1778; however, the different study durations between GNE-617 and GMX-1778 do not allow for direct comparison of retinal toxicity.
相关产品:Bioactive Compound Library Plus | Metabolism/Protease Compound Library | Anti-Cancer Compound Library | Anti-Lung Cancer Compound Library | Human Metabolite Library | Heterocyclic Compound Library | Highly Selective Inhibitors Library | OT-82 | SBI-797812 | CB 300919 | GNE-617 | NAT | Nampt degrader-2 | GNE-618 | Nampt-IN-10 trihydrochloride | Nampt-IN-5 | NAMPT degrader-1 | CB30865 | GPP78 | NAMPT inhibitor-linker 2 | Nampt-IN-1 | Nampt activator-1 | Teglarinad chloride | LB-60-OF61 hydrochloride | STF-118804 | Nampt-IN-9 | CHS-828 | Nampt activator-3 | LB-60-OF61 | Nampt-IN-3 | Nampt-IN-8 | Nampt-IN-10 TFA | Nampt-IN-7 | (E)-Daporinad | Nampt activator-2 | NAMPT/IDO1-IN-1
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货号: HY-15766A
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