| Identification | Back Directory | [Name]
5-([1,1'-biphenyl]-4-ylmethylene)-2-[4-(2-hydroxyethyl)-1-piperazinyl]-1,3-thiazol-4(5H)-one | [CAS]
678158-55-9 | [Synonyms]
Mcl1-IN-8
Mcl-1-Puma inhibitor 8
5-([1,1'-biphenyl]-4-ylmethylene)-2-[4-(2-hydroxyethyl)-1-piperazinyl]-1,3-thiazol-4(5H)-one | [Molecular Formula]
C22H23N3O2S | [MDL Number]
MFCD09857618 | [MOL File]
678158-55-9.mol | [Molecular Weight]
393.5 |
| Chemical Properties | Back Directory | [Boiling point ]
596.6±60.0 °C(Predicted) | [density ]
1.27±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 50 mg/mL (127.06 mM) | [form ]
Solid | [pka]
14.96±0.10(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Description]
Mcl-1-PUMA modulator-8 is a modulator of Mcl-1-PUMA interaction which suppresses cancer cells and inhibits PUMA-dependent apoptosis of non-cancerous cells. | [Uses]
CLZ-8 (Compound 8) is an orally active Mcl-1-PUMA interface inhibitor, with a Ki of 0.3 μM. CLZ-8 exhibits dual activity on reduce PUMA-dependent apoptosis while deactivating Mcl-1-mediated anti-apoptosis in cancer cells[1]. | [in vivo]
CLZ-8 (0-400 mg/kg; i.g.; once) shows powerful anti-radiation effects in mice[2]. | Animal Model: | 6-8 week-old male BALB/c mice[2] | | Dosage: | 100, 200 and 400 mg/kg | | Administration: | Intragastric administration, once, 30 min prior to irradiation | | Result: | Increased the survival rate of irradiated mice. |
| [IC 50]
Mcl-1: 0.3 μM (Ki); PUMA | [References]
[1] Liu J, et al. Targeting the apoptotic Mcl-1-PUMA interface with a dual-acting compound. Oncotarget. 2017 Apr 20;8(33):54236-54242. DOI:10.18632/oncotarget.17294
[2] Feng T, et al. CLZ-8, a potent small-molecular compound, protects radiation-induced damages both in vitro and in vivo. Environ Toxicol Pharmacol. 2018 Jul;61:44-51. |
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