| Identification | Back Directory | [Name]
2-[(4-chlorobenzoyl)carbamothioylamino]-4-ethyl-5-methylthiophene-3-carboxamide | [CAS]
925069-34-7 | [Synonyms]
PI-273
2-[(4-chlorobenzoyl)carbamothioylamino]-4-ethyl-5-methylthiophene-3-carboxamide
2-({[(4-chlorobenzoyl)amino]carbonothioyl}amino)-4-ethyl-5-methyl-3-thiophenecarboxamide
3-Thiophenecarboxamide, 2-[[[(4-chlorobenzoyl)amino]thioxomethyl]amino]-4-ethyl-5-methyl- | [Molecular Formula]
C16H16ClN3O2S2 | [MOL File]
925069-34-7.mol | [Molecular Weight]
381.9 |
| Chemical Properties | Back Directory | [density ]
1.425±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 6.25 mg/mL (16.37 mM) | [form ]
Solid | [pka]
8.09±0.70(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
PI-273 is a first reversibly and specific phosphatidylinositol 4-kinase (PI4KIIα) inhibitor with an IC50 of 0.47 μM. PI-273 can inhibit breast cancer cell proliferation, block the cell cycle and induce cell apoptosis[1]. | [in vivo]
PI-273 (intraperitoneal injection; 25 mg/kg/day; 15 days) profoundly suppresses the tumor volume and weight in the MCF-7 xenografts[1].
PI-273 (0.5 mg/kg (intravenously) or 1.5 mg/kg (intragastrically); 0.08-5 hours) has a half-life of 0.411 hours for intravenous administration and 1.321 hours for intragastrical administration, and the absolute bioavailability of PI-273 is 5.1%[1].
| Animal Model: | Eight-week-old male BALB/c nude mice with MCF-7 cell[1] | | Dosage: | 25 mg/kg | | Administration: | Intraperitoneal injection; daily; 15 days | | Result: | Suppressed the tumor volume and weight in the MCF-7 xenografts.
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| Animal Model: | Male Sprague-Dawley (SD) rats[1] | | Dosage: | 0.5 mg/kg (intravenously) or 1.5 mg/kg (intragastrically) (Pharmacokinetic Study) | | Administration: | Intravenously or intragastrically; 0.08, 0.16, 0.33, 0.67, 1, 1.5, 2, 3 and 5 hours | | Result: | Has a half-life of 0.411 hours for intravenous administration and 1.321 hours for intragastrical administration, and the absolute bioavailability of PI-273 is 5.1%.
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| [IC 50]
PI4KIIα: 0.47 μM (IC50) | [storage]
Store at -20°C | [References]
[1] Li J, et al. PI-273, a Substrate-Competitive, Specific Small-Molecule Inhibitor of PI4KIIα, Inhibits the Growth of Breast Cancer Cells. Cancer Res. 2017 Nov 15;77(22):6253-6266. DOI:10.1158/0008-5472.CAN-17-0484 |
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