315703-52-7 Usage
Description
N-(4-Ethoxyphenyl)-4-(2-methylimidazo[1,2-a]pyridin-3-yl)thiazol-2-amine, also known as JK 184, is an imidazopyridine derivative that functions as a small molecule antagonist of the Hedgehog (Hh) signaling pathway. It is characterized by its ability to inhibit downstream hedgehog signaling, which prevents Gli-dependent transcriptional activity with an IC50 of 30 nM. N-(4-Ethoxyphenyl)-4-(2-methylimidazo[1,2-a]pyridin-3-yl)thiazol-2-amine also inhibits alcohol dehydrogenase 7 (IC50 = 210 nM) and depolymerizes microtubules, preventing their assembly, which is essential for Gli function.
Uses
Used in Pharmaceutical Industry:
N-(4-Ethoxyphenyl)-4-(2-methylimidazo[1,2-a]pyridin-3-yl)thiazol-2-amine is used as an antiproliferative agent for various cancer cell lines, including L3.6pl, Panc 05.04, BxPC3, D283 med, and Daoy, with GI50s ranging from 3-21 nM. It is particularly effective in L3.6pl and BxPC3 pancreatic cancer xenograft models, where it demonstrates significant antitumor activity at a dosage of 0.2 mg/mouse/day.
Used in Cancer Research:
In the field of cancer research, N-(4-Ethoxyphenyl)-4-(2-methylimidazo[1,2-a]pyridin-3-yl)thiazol-2-amine serves as a valuable tool for studying the Hedgehog signaling pathway and its role in cancer development and progression. By targeting this pathway, researchers can gain insights into the molecular mechanisms underlying cancer growth and identify potential therapeutic targets for the development of novel anticancer drugs.
Used in Drug Development:
N-(4-Ethoxyphenyl)-4-(2-methylimidazo[1,2-a]pyridin-3-yl)thiazol-2-amine is utilized in drug development as a lead compound for the design and synthesis of new Hedgehog pathway antagonists. Its unique mechanism of action and potent inhibitory effects on Gli-dependent transcriptional activity make it a promising candidate for the development of targeted therapies against various cancers driven by aberrant Hedgehog signaling.
Biological Activity
Potent downstream hedgehog (Hh) signaling inhibitor that prevents Gli-dependent transcriptional activity (IC 50 = 30 nM). Exhibits antiproliferative activity in a range of cancer cell lines (GI 50 = 3 - 21 nM) and in human xenografts in vivo . Inhibits alcohol dehydrogenase 7 (Adh7) (IC 50 = 210 nM) and acts as a microtubule depolymerizing agent in vitro .
Check Digit Verification of cas no
The CAS Registry Mumber 315703-52-7 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 3,1,5,7,0 and 3 respectively; the second part has 2 digits, 5 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 315703-52:
(8*3)+(7*1)+(6*5)+(5*7)+(4*0)+(3*3)+(2*5)+(1*2)=117
117 % 10 = 7
So 315703-52-7 is a valid CAS Registry Number.
315703-52-7Relevant articles and documents
The imidazopyridine derivative JK184 reveals dual roles for microtubules in hedgehog signaling
Cupido, Tommaso,Rack, Paul G.,Firestone, Ari J.,Hyman, Joel M.,Han, Kyuho,Sinha, Surajit,Ocasio, Cory A.,Chen, James K.
, p. 2321 - 2324 (2009)
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COMPOUNDS AND COMPOSITIONS AS HEDGEHOG PATHWAY MODULATORS
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, (2009/09/05)
The invention provides a method for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-fu
