2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. HSP
  4. XL888

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
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 183 In-stock
Solution
10 mM * 1 mL in DMSO USD 183 In-stock
Solid
1 mg USD 55 In-stock
5 mg USD 165 In-stock
10 mg USD 264 In-stock
25 mg USD 495 In-stock
50 mg USD 902 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 3 publication(s) in Google Scholar

XL888 Related Antibodies

Top Publications Citing Use of Products

View All HSP Isoform Specific Products:

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HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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].

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

XL888 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

503.64

Formula

C29H37N5O3
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (99.28 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9855 mL 9.9277 mL 19.8555 mL
5 mM 0.3971 mL 1.9855 mL 3.9711 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.25 mg/mL (2.48 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1.25 mg/mL (2.48 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.39%

COA (248 KB) HNMR (223 KB) LCMS (111 KB)

Handling Instructions (2659 KB)
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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9855 mL 9.9277 mL 19.8555 mL 49.6386 mL
5 mM 0.3971 mL 1.9855 mL 3.9711 mL 9.9277 mL
10 mM 0.1986 mL 0.9928 mL 1.9855 mL 4.9639 mL
15 mM 0.1324 mL 0.6618 mL 1.3237 mL 3.3092 mL
20 mM 0.0993 mL 0.4964 mL 0.9928 mL 2.4819 mL
25 mM 0.0794 mL 0.3971 mL 0.7942 mL 1.9855 mL
30 mM 0.0662 mL 0.3309 mL 0.6618 mL 1.6546 mL
40 mM 0.0496 mL 0.2482 mL 0.4964 mL 1.2410 mL
50 mM 0.0397 mL 0.1986 mL 0.3971 mL 0.9928 mL
60 mM 0.0331 mL 0.1655 mL 0.3309 mL 0.8273 mL
80 mM 0.0248 mL 0.1241 mL 0.2482 mL 0.6205 mL
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XL888 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

XL8881149705-71-4XL 888XL-888HSPHeat shock proteinsInhibitorinhibitorinhibit

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