XMU-MP-3 是一种有效的非共价 BTK 抑制剂，在 10 μM ATP 存在下，对 BTK WT 和 BTK C481S 突变型的 IC₅₀ 分别为 10.7 nM 和 17.0 nM。XMU-MP-3 也诱导凋亡 (apoptosis)。

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.

Solid

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

XMU-MP-3 (0.001-10000 nM; 48 hours) inhibits BTK-transformed Ba/F3 cell proliferation with an IC50 of 11.4 nM.
XMU-MP-3 (1-10000 nM) inhibits the proliferation of JeKo-1, Ramos and NALM-6 with IC50 values of 326.6 nM, 685.6 nM and 1065 nM, respectively.
XMU-MP-3 (0.001-10000 nM) maintains inhibitory potency with an IC50 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. has not independently confirmed the accuracy of these methods. They are for reference only.

XMU-MP-3 (25 and 50 mg/kg) substantially suppresses tumor growth in mouse xenograft models. 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) bearin

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Fu Gui, et al. A Non-Covalent Inhibitor XMU-MP-3 Overrides Ibrutinib-Resistant Btk C481S Mutation in B-cell Malignancies. Br J Pharmacol. 2019 Dec;176(23):4491-4509.

In Vitro: DMSO : 100 mg/mL (186.38 mM; Need ultrasonic)配制储备液