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XL888

Chemical Structure : XL888

CAS No.: 1149705-71-4

XL888 (XL-888, XL 888)

Catalog No.: PC-21234Not For Human Use, Lab Use Only.

XL888 is a potent small molecule inhibitor of HSP90 with IC50 of 24 nM, inhibits cell proliferation of multiple cancer cell types.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

XL888 is a potent small molecule inhibitor of HSP90 with IC50 of 24 nM, inhibits cell proliferation of multiple cancer cell types.
XL888 potently inhibited cell growth, induced apoptosis, and prevented the growth of vemurafenib-resistant melanoma cell lines in 3-dimensional cell culture, long-term colony formation assays, and human melanoma mouse xenografts.
XL888 treatment increased BIM expression, decreased Mcl-1 expression, and induced apoptosis.
XL888 is effective at reversing BRAF inhibitor resistance in melanoma, including that mediated through acquired NRAS mutations.

Physicochemical Properties

M.Wt 503.65
Formula C29H37N5O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1,4-Benzenedicarboxamide, N1-[(3-endo)-8-[5-(cyclopropylcarbonyl)-2-pyridinyl]-8-azabicyclo[3.2.1]oct-3-yl]-2-methyl-5-[[(1R)-1-methylpropyl]amino]-

References

1. Paraiso KH, et al. Clin Cancer Res. 2012 May 1;18(9):2502-14.

2. Bussenius J, et al. Bioorg Med Chem Lett. 2012 Sep 1;22(17):5396-404.

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