Aprutumab ixadotin (Synonyms: BAY 1187982)

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Aprutumab ixadotin (BAY 1187982) is the first antibody-drug conjugate (ADC) to target FGFR2 and the first to use Auristatin-based payload.

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Aprutumab ixadotin Chemical Structure

CAS No. : 1708947-48-1

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Biological Activity
Purity & Documentation
References
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Description

Aprutumab ixadotin (BAY 1187982) is the first antibody-drug conjugate (ADC) to target FGFR2 and the first to use Auristatin-based payload^[1]^[2].

In Vitro

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.

Cell Viability Assay^[1]

Cell Line:	SNU-16, KATO III, SUM-52PE, NCI-H716, and MFM-223 cells; MDA-MB-231 cells; KYSE-180 cells; 4T1 cells
Concentration:	0.097-0.83 nM
Incubation Time:	72 hours
Result:	Inhibited cell viability.

In Vivo

Aprutumab ixadotin (5 mg/kg and 7.5 mg/kg; i.v.; once weekly for 30 d) is well tolerated, and results in partial tumor regression in SNU-16, MFM-223 or NCI-H716 xenograft models in mice^[1].

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

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]
Dosage:	0.5 mg/kg, 1 mg/kg, 5 mg/kg, 7.5 mg/kg, 15 mg/kg
Administration:	Intravenous injection; once weekly for 4 weeks
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.

CAS No.

1708947-48-1

SMILES

[Aprutumab ixadotin]

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Inhibitory Antibodies User Guide (602 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]

Aprutumab ixadotin Related Classifications

Inhibitory Antibodies

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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:

Aprutumab ixadotin1708947-48-1BAY 1187982BAY1187982BAY-1187982Antibody-Drug Conjugates (ADCs)FGFRAntibody-Drug ConjugatesFibroblast growth factor receptorInhibitorinhibitorinhibit

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