Aprutumab ixadotin
Based on 1 Customer Validation
Aprutumab ixadotin (BAY 1187982) is the first antibody-drug conjugate (ADC) to target FGFR2 and the first to use Auristatin-based payload. Aprutumab ixadotin contains a fully human anti-FGFR2 monoclonal antibody (Aprutumab) (HY-P99007) conjugated by lysine side chains to a non-cleavable linker and via this an innovative Auristatin W derivative. Aprutumab ixadotin can be used for the study of advanced solid tumors, such as FGFR2-positive gastric cancer and triple-negative breast cancer.
For research use only. We do not sell to patients.
- Purity: 98.99%
- CAS No.: 1708947-48-1
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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FGFR2 |
Aprutumab ixadotin (0.097-0.83 nM; 72 h) exhibits antigen binding affinity of 0.29 nM against FGFR2, and shows inhibitory activities in several cell lines with IC50s of 0.097-0.83 nM[1].
Aprutumab ixadotin induces apoptosis in vitro specifically in FGFR2-positive cells (SUN-52PE, SUN-16)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SNU-16, KATO III, SUM-52PE, NCI-H716, and MFM-223 cells; MDA-MB-231 cells; KYSE-180 cells; 4T1 cells
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Concentration:0.097-0.83 nM
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Incubation Time:72 hours
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Result:Inhibited cell viability.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SNU-16 xenograft model in female NOD scid mice and MFM-223 and NCI-H716 xenograft models in female NMRI nu/nu mice[1]
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Dosage:0.5 mg/kg, 1 mg/kg, 5 mg/kg, 7.5 mg/kg, 15 mg/kg
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Administration:Intravenous injection; once weekly for 4 weeks
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Result:Significantly tumor growth at least 90% at 5 mg/kg in SNU-16 xenograft model. However, doses of 0.5 or 1 mg/kg did not significantly inhibit tumor growth compared to the vehicle control.
Marked decrease in tumor volume at 1 and 5 mg/kg in MFM-223 model.
Resulted in notable inhibition of tumor growth at 7.5 mg/kg in cell line derived xenograft model overexpressing FGFR2, the NCI-H716 human colorectal cancer model.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1708947-48-1
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Appearance Liquid
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Color Colorless to light yellow
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SMILES
[Aprutumab ixadotin]
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Synonyms
BAY 1187982
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Shipping
Shipping with dry ice.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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Data Sheet (261 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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Handling Instructions (2659 KB)
References
[1]. Sommer A, et al. Preclinical Efficacy of the Auristatin-Based Antibody-Drug Conjugate BAY 1187982 for the Treatment of FGFR2-Positive Solid Tumors. Cancer Res. 2016 Nov 1;76(21):6331-6339. [Content Brief]
[2]. Kim SB, et al. First-in-Human Phase I Study of Aprutumab Ixadotin, a Fibroblast Growth Factor Receptor 2 Antibody-Drug Conjugate (BAY 1187982) in Patients with Advanced Cancer. Target Oncol. 2019 Oct;14(5):591-601. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Aprutumab ixadotin Related Classifications
HY-141600 Related Classifications
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