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

Apatorsen sodium  (Synonyms: OGX-427 sodium)

Cat. No.: HY-145722 Purity: 98.54%
Handling Instructions Technical Support

Apatorsen (OGX-427) sodium is a 2'-methoxyethyl-modified antisense oligonucleotide and also a Hsp27 inhibitor. Apatorsen sodium reduces Hsp27 mRNA and protein levels, impairs stress-induced cytoprotective functions, induces cell apoptosis, inhibits tumor growth and prevents metastasis. Apatorsen sodium 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), nonadecasodium salt

Apatorsen sodium Chemical Structure

CAS No. : 915443-09-3

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Based on 1 publication(s) in Google Scholar

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Description

Apatorsen (OGX-427) sodium is a 2'-methoxyethyl-modified antisense oligonucleotide and also a Hsp27 inhibitor. Apatorsen sodium reduces Hsp27 mRNA and protein levels, impairs stress-induced cytoprotective functions, induces cell apoptosis, inhibits tumor growth and prevents metastasis. Apatorsen sodium 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 sodium (50 nM; transfected for 2 days, treated with erlotinib for 48 h) synergistically enhances erlotinib-induced cell viability reduction and apoptosis in A549 and HCC827 non-small cell lung cancer cells. Apatorsen sodium (12.5-100 nM (treated with pemetrexed); 50 nM (treated with cisplatin, paclitaxel, gemcitabine); treated for 2 days, co-incubated with chemotherapy drugs for 72 h) synergistically enhances the cell viability reduction and apoptosis-promoting effects of pemetrexed, cisplatin, paclitaxel and gemcitabine in A549 non-small cell lung cancer cells.

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

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 sodium (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 (free acid)

CAS No.
Appearance

Solid

Color

Off-white to light yellow

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), nonadecasodium salt

SMILES

[Apatorsen (sodium)]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Purity & Documentation

Purity: 98.54%

References
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    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.

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Apatorsen sodium
Cat. No.:
HY-145722
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