All AbMole products are for research use only, cannot be used for human consumption.
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 |
|---|
| BIIB021
BIIB021 (CNF2024) is an orally available synthetic non-ansamycin Hsp90 inhibitor with ki value of 1.7nM. |
| CUDC-305
CUDC-305 is a heat shock protein 90 (HSP90) inhibitor of the novel imidazopyridine class, with IC50 values of 100 and 103 nM for HSP90α and HSP90β, respectively. |
| Ganetespib
Ganetespib (STA-9090) is a potent synthetic small molecule inhibitor of Hsp90 with potential antineoplastic activity. |
| Luminespib (AUY922)
Luminespib (AUY922) is a small molecule Heat Shock Protein 90 (HSP90) inhibitor with IC50 values of 13 and 21 nM for HSP90α and HSP90β respectively. |
| NVP-HSP990
NVP-HSP990 is an orally bioavailable inhibitor of human heat-shock protein 90 (Hsp90) with IC50 values of 0.6, 0.8, and 8.5 nM for Hsp90α, Hsp90β, and Grp94, respectively. NVP-HSP990 has potential antineoplastic activity. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2026 AbMole BioScience. All Rights Reserved.
