| Identification | Back Directory | [Name]
N-(4-Ethoxyphenyl)-4-(2-methylimidazo[1,2-a]pyridin-3-yl)thiazol-2-amine | [CAS]
315703-52-7 | [Synonyms]
JK 184
CS-2369
JK184 (JK-184
Hh Signaling Antagonist VII
Hh Signaling Antagonist VII, JK184
JK 184;JK-184;HH SIGNALING ANTAGONIST VII
Hh Signaling Antagonist VII, JK184 - CAS 315703-52-7 - Calbiochem
N-(4-Ethoxyphenyl)-4-(2-methylimidazo[1,2-a]pyridin-3-yl)thiazol-2-amine
N-(4-Ethoxyphenyl)-4-(2-methylimidazo[1,2-a]pyridin-3-yl)-2-thiazolamine
2-ThiazolaMine, N-(4-ethoxyphenyl)-4-(2-MethyliMidazo[1,2-a]pyridin-3-yl)- | [Molecular Formula]
C19H18N4OS | [MDL Number]
MFCD01044465 | [MOL File]
315703-52-7.mol | [Molecular Weight]
350.44 |
| Hazard Information | Back Directory | [Uses]
JK 184 is an imidazopyridine derivative that inhibits downstream hedgehog signaling, preventing Gli-dependent transcriptional activity (IC50 = 30 nM). It does so by inhibiting alcohol dehydrogenase 7 (IC50 = 210 nM) and depolymerizing microtubules, preventing their assembly, which is crucial for Gli function. JK 184 exhibits antiproliferative activity in a range of cancer cell lines (L3.6pl, Panc 05.04, BxPC3, D283 med, Daoy; GI50s = 3-21 nM) and in L3.6pl and BxPC3 pancreatic cancer xenograft models (0.2 mg/mouse/day).[Cayman Chemical] | [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 . | [in vivo]
JK184 (5 mg/kg, injected intravenously) exhibits good anti-proliferative activity in subcutaneous Panc-1 and BxPC-3 tumor models, and is a good candidate as antitumor drug targeted Hh signaling. However, JK184 has a poor pharmacokinetic profile and bioavailability[1]. | [storage]
Store at -20°C |
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| Company Name: |
LETOPHARM LIMITED
|
| Telephone: |
+86-21-5821 5861 |
| Website: |
www.letopharm.com |
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