Ponsegromab
Based on 3 publication(s) in Google Scholar
Ponsegromab is a Growth differentiation factor 15 (GDF15) inhibitor with human, cynomolgus monkey, and mouse target IC50 values of 0.123 nM, 0.053 nM, and 0.102 nM, respectively. Ponsegromab acts as a chemosensitizer, increases intracellular reactive oxygen species, reduces glutathione levels. Ponsegromab can be used for the research of oxaliplatin-resistant colorectal cancer.
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- Pureza : 99.60%
- No. CAS: 2368950-15-4
- Peso molecular:145.5 kDa
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Publications Citing Use of MedChemExpress (MCE) Ponsegromab
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Actividad biológica
Descripciòn
Isotype
Human IgG1 (L234A/L235A) kappa
Recommend Isotype Controls
Species Reactivity
Human
IC50 & Target
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GDF15 |
In Vitro
Ponsegromab (log concentrations from -4 to 2 nM; 1 h at 37 °C) potently inhibits the binding of human, cynomolgus monkey, and mouse GDF15 to GFRAL in cell-free ELISA assays with IC50 values of 0.123 nM, 0.053 nM, and 0.102 nM, respectively[1].
Ponsegromab (log concentrations from -4 to 1 nM; 17 h at 37 °C with 5% CO2) potently inhibits GDF15-GFRAL-RET-mediated ELK1 reporter activity in HEK293 cells with an IC50 of 0.037 nM[1].
Ponsegromab (log concentrations from -4 to 2 nM) potently inhibits GDF15-GFRAL-RET-mediated ERK1/2 phosphorylation in HEK293 cells with an IC50 of 0.051 nM[1].
Ponsegromab (log concentrations from -3 to 2 nM) potently inhibits GDF15-GFRAL-RET-mediated AKT phosphorylation in HEK293 cells with an IC50 of 0.171 nM[1].
Ponsegromab (10 µg/mL; 48 h) sensitizes LoVo-OxR and HCT-116-OxR oxaliplatin-resistant colorectal cancer cells to oxaliplatin, reducing oxaliplatin IC50 values to 8.176 μM and 7.818 μM, respectively[2].
Ponsegromab (10 µg/mL; 48 h) increases apoptosis in oxaliplatin-treated LoVo-OxR and HCT-116-OxR oxaliplatin-resistant colorectal cancer cells[2].
Ponsegromab (10 µg/mL; 48 h) modulates apoptosis-related protein expression in oxaliplatin-treated LoVo-OxR and HCT-116-OxR oxaliplatin-resistant colorectal cancer cells, reducing Bcl-2 and increasing cleaved caspase-3 levels[2].
Ponsegromab (10 µg/mL; 48 h) increases oxaliplatin-induced intracellular ROS levels in LoVo-OxR and HCT-116-OxR oxaliplatin-resistant colorectal cancer cells[2].
Ponsegromab (10 µg/mL; 48 h) reduces GSH levels and GSSG/GSH ratio in oxaliplatin-treated LoVo-OxR and HCT-116-OxR oxaliplatin-resistant colorectal cancer cells[2].
Ponsegromab (10 µg/mL; 48 h) reduces protein levels of Nrf2, NQO1, and HO-1 in LoVo-OxR and HCT-116-OxR oxaliplatin-resistant colorectal cancer cells[2].
Ponsegromab (10 µg/mL; 48 h) increases Nrf2 polyubiquitination and reduces Nrf2 interaction with β-TrCP in LoVo-OxR and HCT-116-OxR oxaliplatin-resistant colorectal cancer cells[2].
Ponsegromab (10 µg/mL; 48 h) increases the rate of Nrf2 protein degradation in HCT-116-OxR oxaliplatin-resistant colorectal cancer cells[2].
Ponsegromab (10 µg/mL; 2 h) reduces Nrf2 protein levels via the ubiquitin-proteasome pathway in LoVo-OxR and HCT-116-OxR oxaliplatin-resistant colorectal cancer cells, as MG132 treatment restores Nrf2 expression[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:LoVo-OxR, HCT-116-OxR (oxaliplatin-resistant human colorectal cancer cell lines)
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Concentration:10 µg/mL (in combination with oxaliplatin at 0, 2, 4, 8, 16, 32 μM)
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Incubation Time:48 h
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Result:Reduced the half-maximal inhibitory concentration (IC50) of oxaliplatin in LoVo-OxR cells from 14.290 μM to 8.176 μM, and in HCT-116-OxR cells from 19.650 μM to 7.818 μM, sensitizing the resistant cell lines to oxaliplatin treatment.
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Cell Line:LoVo-OxR, HCT-116-OxR (oxaliplatin-resistant human colorectal cancer cell lines)
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Concentration:10 µg/mL (in combination with 14.29 μM oxaliplatin for LoVo-OxR, 19.65 μM oxaliplatin for HCT-116-OxR)
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Incubation Time:48 h
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Result:Increased the proportion of apoptotic cells in oxaliplatin-treated LoVo-OxR and HCT-116-OxR cells, compared to oxaliplatin treatment alone.
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Cell Line:LoVo-OxR, HCT-116-OxR (oxaliplatin-resistant human colorectal cancer cell lines)
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Concentration:10 µg/mL (in combination with 14.29 μM oxaliplatin for LoVo-OxR, 19.65 μM oxaliplatin for HCT-116-OxR)
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Incubation Time:48 h
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Result:Reduced anti-apoptotic Bcl-2 protein levels and increased pro-apoptotic cleaved caspase-3 protein levels in oxaliplatin-treated LoVo-OxR and HCT-116-OxR cells.
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Cell Line:LoVo-OxR, HCT-116-OxR (oxaliplatin-resistant human colorectal cancer cell lines)
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Concentration:10 µg/mL
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Incubation Time:48 h
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Result:Reduced protein levels of Nrf2, as well as its downstream antioxidant target genes NQO1 and HO-1, in LoVo-OxR and HCT-116-OxR cells.\nIncreased polyubiquitination of Nrf2 and impaired the interaction between Nrf2 and β-TrCP (a ubiquitin ligase adapter) in LoVo-OxR and HCT-116-OxR cells.
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Cell Line:HCT-116-OxR (oxaliplatin-resistant human colorectal cancer cell line)
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Concentration:10 µg/mL
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Incubation Time:48 h (prior to cycloheximide chase over 60 min)
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Result:Increased the rate of Nrf2 protein degradation in HCT-116-OxR cells, reducing the half-life of Nrf2 protein compared to untreated control cells.
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Cell Line:LoVo-OxR, HCT-116-OxR (oxaliplatin-resistant human colorectal cancer cell lines)
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Concentration:10 µg/mL (in combination with 10 μM MG132)
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Incubation Time:2 h
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Result:Reduced Nrf2 protein levels in LoVo-OxR and HCT-116-OxR cells, and this inhibitory effect was reversed by MG132 treatment, restoring Nrf2 expression.
In Vivo
Ponsegromab (10 mg/kg; i.p.; once every 3 days; until study endpoint) restores body weight, increases ambulatory activity, partially normalizes respiratory exchange ratio, and increases heat production in HT-1080 tumor-bearing NCG mice with cancer cachexia[1].
Ponsegromab (10 mg/kg; i.p.; twice weekly; until study endpoint) partially reverses body weight loss in Renca tumor-bearing BALB/c mice with cancer cachexia[1].
Ponsegromab (10 mg/kg; i.p.; twice weekly; until study endpoint) partially reverses body weight loss in MC38-hGDF15 tumor-bearing C57BL/6 mice with cancer cachexia[1].
Ponsegromab (10 mg/kg; i.p.; once every 3 days; day 6 to day 21) maintains body weight, achieves 100% survival, restores gastrocnemius muscle weight, and partially restores epididymal fat weight in cisplatin-treated C57BL/6 mice with chemotherapy-induced cachexia[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NCG mice (6-week-old male; cancer cachexia model via subcutaneous HT-1080 human fibrosarcoma cell inoculation)[1]
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Dosage:10 mg/kg
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Administration:i.p.; twice weekly; until study endpoint
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Result:Increased gastrocnemius muscle weight; significantly increased epididymal fat weight compared to vehicle control.
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Animal Model:NCG mice (6-week-old male; cancer cachexia model via subcutaneous HT-1080 human fibrosarcoma cell inoculation)[1]
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Dosage:10 mg/kg
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Administration:i.p.; once every 3 days; until study endpoint
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Result:Restored lost body weight in cachectic mice; increased ambulatory activity compared to vehicle control; partially restored respiratory exchange ratio towards non-tumor bearing levels; increased heat production compared to vehicle control.
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Animal Model:BALB/c mice (6-week-old male; cancer cachexia model via subcutaneous Renca murine kidney tumor cell inoculation)[1]
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Dosage:10 mg/kg
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Administration:i.p.; twice weekly; until study endpoint
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Result:Led to partial recovery of body weight in cachectic mice, though body weight did not return to non-tumor bearing levels.
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Animal Model:C57BL/6 mice (6-week-old male; cancer cachexia model via subcutaneous MC38-hGDF15 murine colon cancer cell inoculation overexpressing human GDF15)[1]
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Dosage:10 mg/kg
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Administration:i.p.; twice weekly; until study endpoint
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Result:Led to partial recovery of body weight in cachectic mice, though body weight did not return to non-tumor bearing levels.
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Animal Model:C57BL/6 mice (6-week-old male; chemotherapy-induced cachexia model via cisplatin injection)[1]
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Dosage:10 mg/kg
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Administration:i.p.; once every 3 days; day 6 to day 21
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Result:Maintained body weight in cachectic mice (preventing continued weight loss seen in vehicle and isotype control groups), with endpoint body weight similar to normal untreated mice; achieved 100% survival to study endpoint; restored gastrocnemius muscle weight to normal levels; partially restored epididymal fat weight compared to vehicle control.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Gene ID
Accession
Conjugated
Unconjugated
Reconsititution
The product can be reconstituted/diluted with sterile PBS or saline.
Format
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Human IgG1 kappa
Aplicación
ELISA, FACS, Functional assay
Verified Bioactivity
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Immobilized GDF-15 Protein, Human (P.pastoris, His, HY-P75170) can bind Ponsegromab. The EC50 for this effect is 9.7 ng/mL. -
Flow Cytometry analysis of HepG2 cells with Ponsegromab (HY-P99241, red). Cells were fixed with 4% paraformaldehyde and permeabilised with 90% methanol. Then cells were stained with the primary antibody at 1/200 dilution for an hour at 4℃. Goat Anti-Human IgG H&L (AF488) (HY-P83776) was used as the secondary antibody at 1/1,000 dilution for 30 minutes at 4℃. Human IgG1 kappa (HY-P99001, blue) was used as the isotype control, cells without incubation with primary antibody were used as the unlabeled control (black).
Chemical Information
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No. CAS 2368950-15-4
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Appearance Liquid
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Peso molecular 145.5 kDa
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Color Colorless to light yellow
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SMILES
[Ponsegromab]
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Synonyms
PF 06946860
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Envío
Shipping with dry ice.
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (3)
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Journal Impact Factor
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Most Recent
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bioRxiv
2024 Jun 17:2024.06.14.598891. PMID: 38948776
Protocolo
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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ROS/oxidative-stress fluorescent staining
ROS/oxidative-stress fluorescent staining uses cell-permeant fluorogenic probes that become fluorescent after oxidation inside cells or tissues; commonly used examples include DCFH-DA/DCFDA for broad cellular oxidant detection, DHE for superoxide-related signal detection, MitoSOX for mitochondrial superoxide-related signal detection, and CellROX probes for oxidative-stress-associated fluorescence readouts. The assay detects probe oxidation rather than a single ROS species unless the probe and analysis method have been chemically validated for that species. DCFH-DA enters cells, is deacetylated by intracellular esterases to DCFH, and produces fluorescent DCF after oxidation, so the readout is used as an operational measure of total cellular oxidative stress rather than a species-specific ROS measurement. DHE and MitoSOX can report superoxide-related oxidation, but red fluorescence alone can include non-specific ethidium-like oxidation products; HPLC or optimized spectral approaches are
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Inhibitory Antibodies User Guide (603 KB)
Referencias
[1]. Huang Y, et al. GB18-06, a nanobody targeting GDF15, effectively alleviates weight loss and restores physical function in cachexia models. MAbs. 2024;16(1):2416453. [Content Brief]
[2]. Lin H, et al. GDF15 induces chemoresistance to oxaliplatin by forming a reciprocal feedback loop with Nrf2 to maintain redox homeostasis in colorectal cancer. Cell Oncol (Dordr). 2024;47(4):1149-1165. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Ponsegromab Related Classifications
HY-P99241 Related Classifications
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