SKU : MC514812
CAS Number : 1257704-57-6
Molecular Formula : C24H26N6O2S | Molecular Weight : 462.57
Quote RequestPurity | NLT 98% |
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Storage | at 20ºC 2 years |
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Chemical Name | CEP-33779 |
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CAS Number | 1257704-57-6 |
MDL Number | MFCD22683932 |
Molecular Formula | C24H26N6O2S |
Molecular Weight | 462.57 |
CEP-33779 is a novel, selective, and orally bioavailable inhibitor of JAK2 with an IC50 of 1.8±0.6 nM. IC50 & Target: IC50: 1.8±0.6 nM (JAK2)[1] In Vitro: CEP-33779, at nontoxic concentrations, significantly sensitizes overexpression of P-glycoprotein overexpressing multidrug resistance cells to its anticancer substrates. CEP-33779 significantly increases intracellular accumulation and decreases the efflux of doxorubicin by inhibiting the overexpression of P-glycoprotein transport function[3]. In Vivo: CEP-33779 exhibits a favorable PK profile in nude mice, an iv half-life of 1 h, moderate distribution (Vd=2.6 L/kg), and measurable oral exposure with an estimated bioavailability of 33%. It demonstrates antitumor efficacy in the CWR22 xenograft model; oral dosing for 14 days at 30 mg/kg bid results in tumor stasis and partial regressions in 5/10 animals[1]. CEP-33779 administration results in an almost complete shrinkage of tumors in most animals; few remaining tumor nodules were small, poorly vascularized, and had a necrotic appearance. CEP-33779 suppressed activation of NF-κB in tumors[2].
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