JAK2-IN-7 , CAS No.2593402-36-7

CAS: 2593402-36-7 Cat. No.: J647723 Fórmula: C₂₆H₃₃N₇O Peso molecular: 459.59

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Visão geral

JAK2-IN-7 is a selective JAK2 inhibitor with IC 50 s of 3, 11.7, and 41 nM for JAK2 , SET-2, and Ba/F3 V617F cells, respectively. JAK2-IN-7 possesses >14-fold selectivity over JAK1 , JAK3 , FLT3 . JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase and induces tumor cell apoptosis . Antitumor activities

In Vitro

JAK2-IN-7 (compound 13ac) (0-1000 nM; 2 hours) inhibits JAK2 and STAT5 phosphorylation in a dose-dependent manner in SET-2 and Ba/F3-JAK2 V617F cells. JAK2-IN-7 (10-160 nM; 24 hours) induces cell arrest in the G0/G1 phase. JAK2-IN-7 (0.05-1.6 μM; 2 hours) induces apoptosis in SET-2 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Cycle AnalysisCell Line: SET-2 cells Concentration: 10-160 nM Incubation Time: 24 hours Result: Induced cell arrest in the G0/G1 phase in a concentration-dependent manner. Apoptosis AnalysisCell Line: SET-2 cells Concentration: 0.05-1.6 μM Incubation Time: 2 hours Result: Induced apoptosis in SET-2 cells.

In Vivo

JAK2-IN-7 (15-60 mg/kg; p.o.; daily for 16 days) shows potent in vivo antitumor efficacy with 82.3% tumor growth inhibition in the SET-2 xenograft model . JAK2-IN-7 (30-60 mg/kg; p.o.; q.d. for 16 day) significantly ameliorates the disease symptoms in a Ba/F3-JAK2V617F allograft model, with 77.1% normalization of spleen weight, which was more potent than Ruxolitinib . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: SET-2 cell-inoculated xenograft NOD/SCID mouse model Dosage: 15, 30, and 60 mg/kg Administration: Orally daily for 16 days Result: Exhibited a significant tumor growth inhibition of 82.3% without obvious weight change.

Form:Solid

IC50& Target:JAK1 42 nM (IC 50 ) JAK2 3 nM (IC 50 ) JAK3 94 nM (IC 50 ) Tyk2 75 nM (IC 50 ) FLT3 62 nM (IC 50 )

Specifications

Mecanismos bioquímicos e fisiológicos

JAK2-IN-7 is a selective JAK2 inhibitor with IC 50 s of 3, 11.7, and 41 nM for JAK2 , SET-2, and Ba/F3 V617F cells, respectively. JAK2-IN-7 possesses >14-fold selectivity over JAK1 , JAK3 , FLT3 . JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase

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

Nomes e identificadores

• Peso molecular: 459.59

Propriedades químicas e físicas

• Solubilidade: DMSO : 250 mg/mL (543.96 mM; Need ultrasonic)

Perguntas frequentes

How should this product be stored?

Store at ?20 °C. Freezer storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.

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

The CAS Number is 2593402-36-7, the molecular formula is C26H33N7O, and the molecular weight is 459.59 g/mol.

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.