For research use only.

Catalog No.S7122

3 publications

XL888 Chemical Structure

CAS No. 1149705-71-4

XL888 is an ATP-competitive inhibitor of HSP90 with IC50 of 24 nM. Phase 1.

Selleck's XL888 has been cited by 3 publications

1 Customer Review

  • B, XL888 (1 mmol/L, 144 hours) is effective at blocking the growth and survival of vemurafenib-resistant melanoma cell lines grown as 3D collagen-implanted spheroids. Staining shows cell viability, in which green corresponds to live cells and red: dead cells. Magnification×4.

    Clin Cancer Res, 2012, 18(9):2502-2514.. XL888 purchased from Selleck.

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Biological Activity

Description XL888 is an ATP-competitive inhibitor of HSP90 with IC50 of 24 nM. Phase 1.
HSP90 [1]
(Cell-free assay)
24 nM
In vitro

XL888 induces HER2 degradation in NCI-N87 cells with IC50 of 56 nM. XL888 inhibits the proliferation of HER2 over-expressed NCI-N87, HER2 over-expressed BT-474, HER2 over-expressed MDA-MB-453, MET mutated MKN45, B-Raf mutated Colo-205, B-Raf mutated SK-MEL-28, EGFR mutated HN5, EGFR mutated NCI-H1975, PI3K mutated MCF7, and K-Ras mutated A549 with IC50 of 21.8, 0.1, 16.0, 45.5, 11.6, 0.3, 5.5, 0.7, 4.1 and 4.3 nM. [1] XL888 leads to dose-dependent decreases in the growth of vemurafenib-naive and vemurafenib-resistant melanoma cell lines and melanoma cell lines with intrinsic resistance with IC50 of all around 0.1 μM. The growth inhibitory effects of XL888 are associated with induction of either a G1-phase cell-cycle arrest (WM164, M229, M229R, M249, M249R, 1205Lu, and WM39 cell lines) or a G2-M phase cell-cycle arrest (WM164R, 1205LuR, and RPMI 7951 cell lines). XL888 (300 nmol) induces high levels ( > 66%) of apoptosis, and loss of mitochondrial membrane potential (TMRM) in these cell lines. The cytotoxic effects of XL888 are durable with no signs of colony formation observed in any of the cell lines even cultured up to 4 weeks. XL888 treatment (300 nM, 48 hours) leads to the degradation of IGF1R, PDGFRβ, ARAF, CRAF, and cyclin D1 and the inhibition of AKT, ERK, and S6 signaling in all of the cell lines with acquired BRAF inhibitor resistance. treatment of cell lines that are naive, intrinsically resistant, and with acquired vemurafenib resistance. Treatment with XL888 (300 nM) leads to robust time-dependent increases in the expression of HSP70 isoform 1. XL888 (48 hours, 300 nM) treatment increases the expression of BIM-EL, BIM-L, and BIM-S expression in the M229R, 1205LuR, RPMI7951, and WM39 cell lines, induces expression of BIM-L and BIM-S in the WM164R cell line, and BIM-EL in the M249R cell line. [2]

In vivo XL888 (100 mg/kg) significantly induces the regression of, or growth inhibition (50%) of established M229R and 1205LuR xenografts in SCID mice. 15 days of XL888 treatment showes a robust (8.6-fold) increase in intratumoral HSP70 expression compared with controls. XL888 treatment is noted to be proapoptotic in vivo and leads to increased TUNEL staining in M229R xenografts associated with increased expression of BIM and decreased expression of Mcl-1. [2]


Cell Research:[2]
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  • Cell lines: 1205Lu melanoma cells lines
  • Concentrations: ~10 μM
  • Incubation Time: 3 days
  • Method: Cells are plated at a density of 2?05 per mL and left to grow overnight before being treated with increasing concentrations of XL888. After incubation with XL888 for 3 days, Methylthiazolyldiphenyl-tetrazolium bromide (MTT) assays are performed.
    (Only for Reference)
Animal Research:[2]
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  • Animal Models: Melanoma carcinoma xenografts 1205Lu
  • Dosages: 100 mg/kg
  • Administration: 3 times per week by oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (198.55 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 503.64


CAS No. 1149705-71-4
Storage powder
in solvent
Synonyms N/A
Smiles CCC(C)NC1=C(C=C(C(=C1)C(=O)NC2CC3CCC(C2)N3C4=NC=C(C=C4)C(=O)C5CC5)C)C(=O)N

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03095781 Recruiting Drug: XL888|Biological: Pembrolizumab Colorectal Adenocarcinoma|Metastatic Pancreatic Adenocarcinoma|Recurrent Colorectal Carcinoma|Recurrent Pancreatic Carcinoma|Stage III Colorectal Cancer|Stage III Pancreatic Cancer|Stage IIIA Colorectal Cancer|Stage IIIB Colorectal Cancer|Stage IV Colorectal Cancer|Stage IV Pancreatic Cancer|Stage IVA Colorectal Cancer|Stage IVA Pancreatic Cancer|Stage IVB Colorectal Cancer|Stage IVB Pancreatic Cancer|Unresectable Pancreatic Carcinoma Emory University|Merck Sharp & Dohme Corp.|Exelixis July 7 2017 Phase 1
NCT00796484 Terminated Drug: XL888 Cancer Exelixis November 2008 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID