1258861-20-9 Usage
Uses
Different sources of media describe the Uses of 1258861-20-9 differently. You can refer to the following data:
1. Smoothened (Smo) is a GPCR-like receptor that, with Patched, mediates hedgehog (Hh) signaling to regulate gene expression through the Gli transcription factors. LY2940680 is an antitumor agent that binds to the human Smo receptor and inhibits Sonic Hh-induced Gli1 expression (IC50 = ~2.4 nM in vitro). The potential anticancer activity of LY2940680 is currently under clinical investigation.[Cayman Chemical]
2. LY2940680 binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling.
Biological Activity
ly2940680 is a selective inhibitor of smo receptor and thus inhibits hh signaling pathway [1].smoothened(smo) receptor is a member of class f g protein-coupled receptors, which plays an important role in the main transducer of the hedgehog (hh) signaling pathway that implicated in a wide range of developmental and adult processes [2].ly2940680 is a potent smo receptor inhibitor that binds mostly to extracelluar loops and has a different functioning site with the reported smo receptor inhibitor sant-1 which binds to 7tm [2]. when tested with cell lines containing a mutation in the gene encoding smoothened that researchers had previously observed in patient with cancer who developed resistance to vismodegib, ly2940680 inhibited cell proliferation [3].many studies have shown that hh signaling pathway plays a pivotal role in cscs and hh inhibition caused many aspects of transformation attributed to cscs. in patients with basal cell carcinoma and medulloblastoma, ly2940680 showed good efficacy as a monotherapy [1].
references
[1]. justilien, v. and a.p. fields, molecular pathways: novel approaches for improved therapeutic targeting of hedgehog signaling in cancer stem cells. clin cancer res, 2015. 21(3): p. 505-13.[2]. hoch, l., et al., mrt-92 inhibits hedgehog signaling by blocking overlapping binding sites in the transmembrane domain of the smoothened receptor. faseb j, 2015. 29(5): p. 1817-29.[3]. redmond, e.m., et al., investigational notch and hedgehog inhibitors--therapies for cardiovascular disease. expert opin investig drugs, 2011. 20(12): p. 1649-64.
Check Digit Verification of cas no
The CAS Registry Mumber 1258861-20-9 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,2,5,8,8,6 and 1 respectively; the second part has 2 digits, 2 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 1258861-20:
(9*1)+(8*2)+(7*5)+(6*8)+(5*8)+(4*6)+(3*1)+(2*2)+(1*0)=179
179 % 10 = 9
So 1258861-20-9 is a valid CAS Registry Number.
1258861-20-9Relevant articles and documents
A novel and efficient route for synthesis of Taladegib
Guo, Mingliang,Hong, Kwon Ho,Lv, Yongfeng,Ding, Yu,Li, Congcong,Xu, Hua,Qi, Wenxiu,Chen, Junqing,Ji, Min,Cai, Jin
, p. 112 - 115 (2017)
Taladegib (LY-2940680), a small molecule Hedgehog signalling pathway inhibitor, was obtained from N-benzyl-4-piperidone via Borch reductive amination, acylation with 4-fluoro-2-(trifluoromethyl)benzoyl chloride, debenzylation, substitution with 1,4-dichlorophthalazine and Suzuki cross-coupling reaction with 1-methyl-1H-pyrazole-5-boronic acid. The advantages of this synthesis route were the elimination of Boc protection and deprotection and the inexpensive starting materials. Furthermore, the debenzylation reaction was achieved with simplified operational procedure using ammonium formate as hydrogen source that provided high reaction yield. This synthetic procedure was suitable for large-scale production of the compound for biological evaluation and further study.
DISUBSTITUTED PHTHALAZINE HEDGEHOG PATHWAY ANTAGONISTS
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Page/Page column 6, (2010/12/31)
The present invention provides novel 1,4-disubstituted phthalazine hedgehog pathway antagonists useful in the treatment of cancer.
