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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.
| Cell Experiment | |
|---|---|
| Cell lines | vemurafenib naïve and resistant melanoma cell lines and melanoma cell lines |
| Preparation method | Growth inhibition. Cells were plated at a density of 2.5 × 104 cells per ml and left to grow overnight before being treated with increasing concentrations of vemurafenib or XL888 as described in (19). Data show the mean of at least three independent experiments ± the S.E. mean. |
| Concentrations | 1nM ~ 10 µM |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | BALB SCID mice bearing Xenograft experiments |
| Formulation | 10mM HCl |
| Dosages | 100 mg/kg 3x per week |
| Administration | oral gavage |
| Molecular Weight | 503.64 |
| Formula | C29H37N5O3 |
| CAS Number | 1149705-71-4 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related HSP Products |
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NCT-58 is a potent inhibitor of C-terminal HSP90. |
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Gedunin is a limonoid with anti-cancer, anti-viral, anti-inflammatory and insecticidal activities. |
| VER-49009
VER-49009 is a Hsp90 inhibitor, with an IC50 of 25 nM and a Kd of 78 nM. |
| YUM70
YUM70 is a potent and selective inhibitor of glucose-regulated protein 78 (GRP78), with an IC50 of 1.5 μM for inhibiting GRP78 ATPase activity. YUM70 induces endoplasmic reticulum stress-mediated apoptosis in pancreatic cancer. |
| Hsp70-derived octapeptide
Hsp70-derived octapeptide is a conserved octapeptide of the C-terminal end of Hsp70, which physically interacts with tetratricopeptide repeat (TPR) motifs. |
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