I-BET567 - ≥99% , CAS No.1887237-54-8

CAS: 1887237-54-8 Cat. No.: I648937 Fórmula: C₁₇H₁₈ClN₅O₂ Peso molecular: 359.81

GRADE & PURITY ≥99%

Storage

Protected from light,Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

I-BET567 is a potent and orally active inhibitor of pan-BET candidate with pIC 50 s of 6.9 and 7.2 for BRD4 BD1 and BD2 , respectively. I-BET567 has been demonstrated efficacy in mouse models of oncology and inflammation

In Vitro

I-BET567 (compound 27) (72 hours; 1.5 nM-30 μM) effectively inhibites the proliferation of human NMC cell line 11060 in vitro with a mean gpIC 50 6.2 (0.63 μM). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: NMC line 11060 cells Concentration: 1.5 nM-30 μM Incubation Time: 72 hours Result: Significantly reduced cell growth.

In Vivo

I-BET567 (compound 27) (3, 10, and 30 mg/kg; p.o.; once daily for 20 days) leads to a significant reduction in tumor growth compared with vehicle controls at both 10 and 30 mg/kg . Assessment of Pharmacokinetics (PK) profile of I-BET567 following intravenous infusion and oral administration in male wistar han rat and beagle dog a . species dose iv b /po c (mg/kg) CL b (mL/min/kg) CL b,u (mL/min/kg) CL renal (mL/min/kg) V ss (L/kg) V ss,u (L/kg) t 1/2 (h) Fpo (%) f ub rat 1.3/3 25 109 7 2.4 10.4 1.6 99 d 0.23 dog 1.0/3 8.1 20 6.9 1.2 2.9 1.8 98 0.41 a: Values are mean, n=3 unless otherwise stated. b: IV dose 1h infusion in DMSO and (10%, w/v) Kleptose HPB in saline (2%: 98% (v/v)). c: PO dose vehicle: 1%(w/v) methycellulose (400 cps) (aq). d: Mean n = 2. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: NMC 11060 xenograft mouse model (NOD/SCID mouse; bearing NMC 11060 cells) Dosage: 3, 10, and 30 mg/kg Administration: p.o. (once daily for 20 days Result: Led to a significant reduction in tumor growth compared to vehicle controls at both 10 and 30 mg/kg.

Form:Solid

IC50& Target:BRD4 (BD1) 6.9 (pIC 50 ) BRD2 7.2 (pIC 50 )

Specifications

Especificaciones y pureza

≥99%

Mecanismos bioquímicos y fisiológicos

I-BET567 is a potent and orally active inhibitor of pan-BET candidate with pIC 50 s of 6.9 and 7.2 for BRD4 BD1 and BD2 , respectively. I-BET567 has been demonstrated efficacy in mouse models of oncology and inflammation.

Condiciones de almacenamiento de almacenamiento

Protected from light,Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Tipo de acción

INHIBITOR

Pureza

≥99%

Nombres e identificadores

Peso molecular

359.81

Propiedades químicas y físicas

• Solubilidad: DMSO : 100 mg/mL (277.92 mM; Need ultrasonic)

Preguntas frecuentes

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1887237-54-8, the molecular formula is C17H18ClN5O2, and the molecular weight is 359.81 g/mol.

What is the purity of this product?

This product is supplied at ≥99% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.

How should this product be stored?

Store at ?80 °C, protected from light. The material is light-sensitive — keep it in its original opaque or amber container.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.