XMU-MP-3 - 10mM in DMSO , CAS No.2031152-08-4

CAS: 2031152-08-4 Cat. No.: X654902 Formula: C₂₇H₂₇F₃N₈O Peso molecolare: 536.55

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Panoramica

XMU-MP-3 is a potent non-covalent BTK inhibitor with IC 50 s of 10.7 nM and 17.0 nM for BTK WT and BTK C481S mutation in the presence of 10 μM ATP, respectively. XMU-MP-3 also induces apoptosis

In Vitro

XMU-MP-3 (0.001-10000 nM; 48 hours) inhibits BTK-transformed Ba/F3 cell proliferation with an IC 50 of 11.4 nM. XMU-MP-3 (1-10000 nM) inhibits the proliferation of JeKo-1, Ramos and NALM-6 with IC 50 values of 326.6 nM, 685.6 nM and 1065 nM, respectively. XMU-MP-3 (0.001-10000 nM) maintains inhibitory potency with an IC 50 of 182.3 nM against BTK(C481S)-Ba/F3 cells. XMU-MP-3 (5000 nM) induces apoptosis in BTK (C481S) Ba/F3 cells. XMU-MP-3 (10-1000 nM; 4 hours) inhibits both the auto- and trans-phosphorylation of BTK at the site of Y223 and Y551 in a dose-dependent manner in BTK-transformed Ba/F3 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: BTK-transformed and parental Ba/F3 cells Concentration: 0.001, 0.01, 0.1, 1, 10, 100, 1000, 10000 nM Incubation Time: 48 hours Result: Inhibited BTK-transformed Ba/F3 cell proliferation with an IC 50 of 11.4 nM, while it showed negligible anti-proliferative effects on parental wild-type Ba/F3 cells (IC 50 >10000 nM). Western Blot AnalysisCell Line: BTK-transformed Ba/F3 cells Concentration: 10, 50, 100, 500, 1000 nM Incubation Time: 4 hours Result: The phosphorylation levels of BTK Y223 and Y551 were reduced significantly at concentrations as low as 100 nM, and completely suppressed at the concentration of 1000 nM.

In Vivo

XMU-MP-3 (25 and 50 mg/kg) substantially suppresses tumor growth in mouse xenograft models . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Nu/nu BALB/c mice (4-6 weeks of age) bearing BTK-transformed Ba/F3 and Ramos xenograft models Dosage: 25 and 50 mg/kg Administration: Treated by tail vein injection; the injection volume was 0.1 mL per 10 g; daily for 14 days Result: Significantly reduced the tumor size without affecting animal weights.

IC50& Target:IC50: 10.7 nM (BTK WT), 17.0 nM (BTK C481S), Apoptosis

Specifications

Specifiche e purezza

10mM in DMSO

Meccanismi biochimici e fisiologici

XMU-MP-3 is a potent non-covalent BTK inhibitor with IC 50 s of 10.7 nM and 17.0 nM for BTK WT and BTK C481S mutation in the presence of 10 μM ATP, respectively. XMU-MP-3 also induces apoptosis.

Condizioni di conservazione di stoccaggio

Store at -80°C

Spedito in

Dry ice packs + Cold packs

Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.

Nomi e identificatori

• Peso molecolare: 536.55

Domande frequenti

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

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 2031152-08-4, the molecular formula is C27H27F3N8O, and the molecular weight is 536.55 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.