2. Antibody-drug Conjugate/ADC Related Protein Tyrosine Kinase/RTK
  3. Antibody-Drug Conjugates (ADCs) FGFR
  4. Aprutumab ixadotin

Aprutumab ixadotin  (Synonyms: BAY 1187982)

Cat. No.: HY-141600

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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

Aprutumab ixadotin Chemical Structure

CAS No. : 1708947-48-1

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Aprutumab ixadotin Related Antibodies

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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.

Aprutumab ixadotin Related Antibodies

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.
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[Aprutumab ixadotin]
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Aprutumab ixadotin Related Classifications

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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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