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BioChemicals
XL888
tcsc0003194
XL888
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AVAILABLE SIZES
1mg
5mg
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25mg
50mg
$
71.00
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ORDERING INFORMATION
International
TAICLONE BIOTECH CORP.
order@taiclone.com
+886-2-2735-9682
+886-2-2735-9807
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Product Description
XL888 is a heat shock protein-90 (
HSP90
) inhibitor, with an
IC
50
of 24 nM.
IC50 & Target: IC50: 24 nM (HSP90)
[3]
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 IC
50
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]
.
Information
CAS No
1149705-71-4
Formula
C
29
H
37
N
5
O
3
Clinical Information
clinicalinformation
Pathway
Metabolic Enzyme/Protease
Cell Cycle/DNA Damage
Target
HSP
HSP
Specifications
Purity / Grade
>98%
Solubility
10 mM in DMSO
Smiles
smiles
Misc Information
Observed Molecular Weight
503.64
related data
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