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Home > Inhibitors & Agonists > Proteasome/Ubiquitin > Heat Shock Protein (HSP)

XL888

  Cat. No.:  DC6307   Featured
Chemical Structure
1149705-71-4
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More than 5000 active chemicals with high quality for research!
Field of application
XL888 is an orally bioavailable, ATP-competitive, small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1149705-71-4
Chemical Name: 5-((R)-sec-butylamino)-N1-((1R,3s,5S)-8-(5-(cyclopropanecarbonyl)pyridin-2-yl)-8-azabicyclo[3.2.1]octan-3-yl)-2-methylterephthalamide
Synonyms: XL888; XL-888; XL 888
SMILES: CCC(C)NC1=CC(=C(C=C1C(=O)N)C)C(=O)NC2C[C@H]3CC[C@@H](C2)N3C4=NC=C(C=C4)C(=O)C5CC5
Formula: C29H37N5O3
M.Wt: 503.28964
Sotrage: 2 years -20°C powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: XL888 is a heat shock protein-90 (HSP90) inhibitor, with an IC50 of 24 nM.
In Vivo: Treatment of the established M245 tumors with XL888 (125 mg/kg 3× week) leads to a significant slowing of tumor growth (P=0.017) without any effect upon animal weights. Analysis of xenograft specimens by LC-MRM shows a marked increase in intratumoral HSP70 expression following XL888 treatment[1]. It is noted that the XL888 is well tolerated by the mice, with no significant alterations in body weigh observed over the study period. LC-MRM mediated analysis of xenograft samples following 15-days of XL888 treatment shows a robust (8.6-fold) increase in intratumoral HSP70 expression compare to controls[2].
In Vitro: XL888 is a heat shock protein-90 (HSP90) inhibitor. Treatment with XL888 leads to dose dependent decreases in the growth of all the cell lines with no significant difference in IC50 values observed between the naive and resistance pairs of cell lines (t=0.25, p=0.82). Treatment of all of the vemurafenib resistant cell lines with XL888 (300 nM) induces high levels (>66%) of apoptosis, caspase-3 cleavage and loss of mitochondrial membrane potential (TMRM) in every cell line tested. Treatment of cell lines that are naïve, intrinsically resistant and with acquired vemurafenib resistance with XL888 (300 nM) leads to robust time-dependent increases in the expression of HSP70 isoform 1 (HSP71)[2].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC70662 NPX-800 NPX-800 is a potent, selective, oral heat shock factor 1 (HSF1) pathway inhibitor.
DC8142 TAS-116 TAS-116 is a highly selective inhibitor of heat shock protein 90α and β, demonstrates potent antitumor activity and minimal ocular toxicity in preclinical models.
DC6307 XL888 XL888 is an orally bioavailable, ATP-competitive, small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity.
DC8299 VER155008 VER-155008 is a novel, small molecule inhibitor of Hsc70/Hsp70 with GI50 of 5.3-14.4 uM in human breast and colon cancer cell lines.
DC9948 SNX-5422(PF04929113) PF-04929113 (SNX-5422) is a potent and selective Hsp90 inhibitor (Kd of 41 nM). PF-04929113 also inhibits Her-2 degradation (IC50 of 37 nM).
DC4118 NVP-BEP800 NVP-BEP800 is a novel, fully synthetic HSP90β inhibitor with IC50 of 58 nM.
DC9994 ML-346 ML346 is a novel activator of Hsp70 with EC50 of 4600 nM in HeLa cell toxicity assay.
DC9963 Kribb11 KRIBB11 is a Heat shock factor (HSF) inhibitor (IC50 = 1.2 μM).
DC8247 KNK437 KNK437 is a pan-HSP inhibitor, which inhibits the synthesis of inducible HSPs, including HSP105, HSP72, and HSP40.
DC10852 KBU2046 KBU2046, is a small molecule that attaches to tumor proteins involved in metastasis and disables them, so they can’t travel to distant organs.
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