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

Apatorsen is a 2'-methoxyethyl-modified antisense oligonucleotide and also a Hsp27 inhibitor. Apatorsen reduces Hsp27 mRNA and protein levels, impairs stress-induced cytoprotective functions, induces cell apoptosis, inhibits tumor growth and prevents metastasis. Apatorsen is applicable to research related to non-small cell lung cancer, castration-resistant prostate cancer, breast cancer, ovarian cancer and bladder cancer.

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

DNA, d(P-thio)([2′-O-(2-methoxyethyl)]rG-[2′-O-(2-methoxyethyl)]rG-[2′-O-(2-methoxyethyl)]rG-[2′-O-(2-methoxyethyl)]rA-m5C-G-m5C-G-G-m5C-G-m5C-T-m5C-G-G-[2′-O-(2-methoxyethyl)]m5rU-[2′-O-(2-methoxyethyl)]m5rC-[2′-O-(2-methoxyethyl)]rA-[2′-O-(2-methoxyethyl)]m5rU)

Apatorsen Chemical Structure

CAS No. : 1002331-21-6

Size Price Stock Quantity
1 mg In-stock
5 mg In-stock
10 mg In-stock
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Apatorsen:

Apatorsen Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Apatorsen

View All HSP Isoform Specific Products:

View All Isoforms
HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Apatorsen is a 2'-methoxyethyl-modified antisense oligonucleotide and also a Hsp27 inhibitor. Apatorsen reduces Hsp27 mRNA and protein levels, impairs stress-induced cytoprotective functions, induces cell apoptosis, inhibits tumor growth and prevents metastasis. Apatorsen is applicable to research related to non-small cell lung cancer, castration-resistant prostate cancer, breast cancer, ovarian cancer and bladder cancer[1][2].

In Vitro

Apatorsen (50 nM; 2 days transfection, 48 h erlotinib co-treatment) synergistically enhances erlotinib-induced reduction in cell viability and apoptosis in A549 and HCC827 non-small cell lung cancer cells[1].
Apatorsen (12.5-100 nM (pemetrexed co-treatment); 50 nM (cisplatin, paclitaxel, gemcitabine co-treatment); 2 days treatment, 72 h chemotherapeutic co-incubation) synergistically enhances the cell viability-reducing and pro-apoptotic effects of pemetrexed, cisplatin, paclitaxel, and gemcitabine in A549 non-small cell lung cancer cells[1].

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

Apatorsen Related Antibodies

Cell Viability Assay[1]

Cell Line: A549, HCC827 non-small cell lung cancer cells
Concentration: 50 nM
Incubation Time: 2 days (transfection); 48 h (erlotinib co-treatment)
Result: Reduced Hsp27 protein expression. Caused greater reduction in cell viability than single-agent treatment when combined with erlotinib. Confirmed a synergistic effect with erlotinib at ED50, ED75, and ED90 for both cell lines. Increased levels of cleaved PARP and cleaved caspase-3 when combined with erlotinib. Increased the subG0 apoptotic cell fraction as measured by flow cytometry when combined with erlotinib.

Cell Viability Assay[1]

Cell Line: A549 non-small cell lung cancer cells
Concentration: 12.5-100 nM (pemetrexed co-treatment); 50 nM (cisplatin, paclitaxel, gemcitabine co-treatment)
Incubation Time: 2 days (OGX-427 treatment); 72 h (chemotherapeutic co-incubation)
Result: Reduced cell viability more than single-agent treatment when combined with pemetrexed. Confirmed synergistic effects with pemetrexed at ED50, ED75, and ED90. Enhanced the cell viability-reducing effects of cisplatin, paclitaxel, and gemcitabine compared to single-agent treatment. Increased levels of cleaved PARP when combined with pemetrexed, cisplatin, paclitaxel, or gemcitabine.
In Vivo

Apatorsen (OGX-427) (15 mg/kg; i.p.; once daily for 7 days then three times weekly; 7 weeks) in combination with erlotinib significantly inhibits A549 xenograft growth and increases tumor apoptosis in male athymic nude mice[1].

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

Animal Model: athymic nude mice (6-8-week-old male; non-small cell lung cancer xenograft model with A549 cells)[1]
Dosage: 15 mg/kg
Administration: i.p.; once daily for 7 days, then three times per week; 7 weeks
Result: Reduced tumor Hsp27 protein levels.
Significantly reduced A549 xenograft growth rates when combined with erlotinib compared to scrambled control plus diluent, scrambled control plus erlotinib, and OGX-427 plus diluent.
Increased average number of TUNEL-positive apoptotic cells when combined with erlotinib compared to control groups.
Molecular Weight

7157.00

CAS No.
Appearance

Solid

Color

White to off-white

Sequence

DNA, d(P-thio)([2′-O-(2-methoxyethyl)]rG-[2′-O-(2-methoxyethyl)]rG-[2′-O-(2-methoxyethyl)]rG-[2′-O-(2-methoxyethyl)]rA-m5C-G-m5C-G-G-m5C-G-m5C-T-m5C-G-G-[2′-O-(2-methoxyethyl)]m5rU-[2′-O-(2-methoxyethyl)]m5rC-[2′-O-(2-methoxyethyl)]rA-[2′-O-(2-methoxyethyl)]m5rU)
SMILES

[Apatorsen]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : ≥ 20 mg/mL (2.79 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.1397 mL 0.6986 mL 1.3972 mL
5 mM --- --- ---
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • 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 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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation
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 (sealed storage, away from moisture). 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
H2O 1 mM 0.1397 mL 0.6986 mL 1.3972 mL 3.4931 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Apatorsen 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:

Apatorsen1002331-21-6OGX-427OGX427OGX 427HSPHeat shock proteinsbladder cancerapoptosisbreast cancerNSCLC cellstumor growthnon-small cell lung cancercastration-resistant prostate cancermetastasisovarian cancerHsp27Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Apatorsen
Cat. No.:
HY-145722A
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (252 KB) Français - FR (252 KB) Deutsch - DE (252 KB) Norwegian - NO (252 KB) Español - ES (252 KB) Swedish - SV (252 KB) Italian - IT (252 KB) Korean - KR (252 KB) Portuguese - PT (252 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.