1. Cell Cycle/DNA Damage
    Metabolic Enzyme/Protease
  2. HSP

XL888 

Cat. No.: HY-13313 Purity: 99.24%
Handling Instructions

XL888 is a heat shock protein-90 (HSP90) inhibitor, with an IC50 of 24 nM.

For research use only. We do not sell to patients.

XL888 Chemical Structure

XL888 Chemical Structure

CAS No. : 1149705-71-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 166 In-stock
Estimated Time of Arrival: December 31
1 mg USD 50 In-stock
Estimated Time of Arrival: December 31
5 mg USD 150 In-stock
Estimated Time of Arrival: December 31
10 mg USD 240 In-stock
Estimated Time of Arrival: December 31
25 mg USD 450 In-stock
Estimated Time of Arrival: December 31
50 mg USD 820 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

View All HSP Isoform Specific Products:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

XL888 is a heat shock protein-90 (HSP90) inhibitor, with an IC50 of 24 nM.

IC50 & Target[3]

HSP90

24 nM (IC50)

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].

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].

Clinical Trial
References
Cell Assay
[1]

Cells are plated in 96-well plates at 2×104 per well. Media with vehicle (DMSO) or XL888 (10, 30, 100 or 300 nM) is added the following day and replaced twice a week. After 4 weeks the plates are stained with crystal violet[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

BALB SCID mice are subcutaneously injected with 2.5×106 cells per mouse and grown to approximately 100 mm3 prior to dosing. Mice are treated with either XL888 100 mg/kg (n=5) or an equivalent volume of vehicle (10 mM HCl), 3× per week by oral gavage. Mouse weights and tumor volumes (L×W2/2) are measured 3× per week. Upon completion of the experiment, vehicle and drug treated tumor biopsies are processed for LC-MRM analysi[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

503.64

Formula

C₂₉H₃₇N₅O₃

CAS No.

1149705-71-4

SMILES

CC1=CC(C(N)=O)=C(N[[email protected]](C)CC)C=C1C(N[[email protected]]2([H])C[[email protected]](CC3)N(C4=NC=C(C(C5CC5)=O)C=C4)[[email protected]]3C2)=O

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
XL888
Cat. No.:
HY-13313
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XL888

Cat. No.: HY-13313