XL888  1149705-71-4

XL-888
分子式：C29H37N5O3    分子量：503.64
 
產(chǎn)品描述
XL888是一種ATP競(jìng)爭(zhēng)性的HSP90 抑制劑，IC50為24nM。
靶點(diǎn)
 HSP90          
IC50
 24 nM           
生物活性
XL888 is an orally bioavailable, ATP-competitive HSP90 inhibitor with potential antineoplastic activity. XL888 specifically binds to Hsp90, inhibiting its chaperone function and promoting the proteasomal degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival. XL888 potently inhibited cell growth, induced apoptosis, and prevented the growth of vemurafenib-resistant melanoma cell lines in vitro and in vivo. XL888 (100 mg/kg) significantly induces the regression or growth inhibition (50%) of established M229R and 1205LuR xenografts in SCID mice. XL888 treatment increased BIM expression, decreased Mcl-1 expression, and induced apoptosis more effectively than dual mitogen-activated protein-extracellular signal-regulated kinase/phosphoinositide 3-kinase (MEK/PI3K) inhibition.
溶解性
可溶于DMSO
穩(wěn)定性
2年 -20°C粉狀，6月-80°C溶于DMSO