EEDi-5285 - ≥99% , CAS No.2488952-40-3

CAS: 2488952-40-3 Cat. No.: E647281 Fórmula: C₂₄H₂₂FN₅O₃S Peso molecular: 479.53

GRADE & PURITY ≥99%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Visão geral

EEDi-5285 is an exceptionally potent and orally active embryonic ectoderm development (EED) inhibitor with an IC 50 value of 0.2 nM for binds to the EED protein. EEDi-5285 has anti-cancer activity

In Vitro

EEDi-5285 inhibits cell growth with IC 50 values of 20 pM and 0.5 nM in the Pfeiffer and KARPAS422 lymphoma cell lines, respectively, carrying an EZH2 mutation. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

EEDi-5285 (compound 28; 50-100 mg/kg; oral gavage; daily; for 28 days; SCID mice) treatment achieves complete and durable tumor regression in the KARPAS422 xenograft model in mice with oral administration . A single 100 mg/kg oral administration of EEDi-5285 (compound 28) effectively reduces the level of H3K27me3 at 24 h in KARPAS422 tumor tissue in mice . EEDi-5285 (compound 28) achieves a C max of 1.8 μM and an AUC of 6.0 h▪μg/ml with 10 mg/kg oral administration and has an oral bioavailability (F) of 75%. EEDi-5285 has a moderate volume of distribution of 1.4 L/kg and a terminal T 1/2 of approximately 2 h . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: SCID mice injected with KARPAS422 cells Dosage: 50 mg/kg, 100 mg/kg Administration: Oral gavage; daily; for 28 days Result: Showed highly efficacious and capable of achieving complete and long-lasting tumor regression in the KARPAS422 xenograft model in mice with oral administration.

Form:Solid

IC50& Target:IC50: 0.2 nM (Embryonic ectoderm development (EED))

Specifications

Especificações e pureza

≥99%

Mecanismos bioquímicos e fisiológicos

EEDi-5285 is an exceptionally potent and orally active embryonic ectoderm development (EED) inhibitor with an IC 50 value of 0.2 nM for binds to the EED protein. EEDi-5285 has anti-cancer activity.

Condições de armazenamento de armazenamento

Store at -20°C

Enviado em

Ice chest + Ice pads

Este produto requer transporte de cadeia fria. Serviços terrestres e outros serviços econômicos não estão disponíveis.

Tipo de ação

INHIBITOR

Pureza

≥99%

Nomes e identificadores

• Peso molecular: 479.53

Propriedades químicas e físicas

• Solubilidade: DMSO : 125 mg/mL (260.67 mM; Need ultrasonic)