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编 号:F744817
分子式:C55H86N10O11
分子量:1063.33
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BAY 1135626 is used to synthesize BAY 1129980, and use to anti-tumor research. BAY 1129980 is a Auristatin-based anti-C4.4A (LYPD3) antibody–agent conjugate (ADC), is used to non–small cell lung cancer (NSCLC) research.

体内研究:
BAY 1129980 (1.9-7.5 mg/kg; i.v.; 20 d) inhibits tumor growth in vivo in mouse.BAY 1129980 with a repeated dosing (15 mg/kg; i.v.; 21 d for 1st cycle and 57 d for 2nd cycle) is well tolerated without changing the sensitivity to the treatment.Animal Model:C4.4A-positive NCI-H292 NSCLC xenograft mouse model
Dosage:1.9, 3.75, 7.5 mg/kg
Administration:Intravenous injection; 20 days
Result:Halted tumor growth on day 20 dose dependently, as the monotherapy treatment, with a minimum effective dose (MED) of 1.9 mg/kg.
Animal Model:C4.4A-positive NCI-H292 NSCLC xenograft mouse model
Dosage:15 mg/kg
Administration:Intravenous injection; 21 days for the first cycle teament, 57 days for the second cycle treatment
Result:Reduced tumor volume with a marked delay of tumor growth.Demonstrated well tolerance, still left regrown tumors sensitive to treatment.

体外研究:
C4.4A (LYPD3) is a protein expressed in non-small cell lung cancer (NSCLC), with scarcely expressing in normal tissues.BAY 1135626 can be synthesized into BAY 1129980 (C4.4A-ADC), shows a strong anti-proliferative effect on C4.4A expressing cell lines. BAY 1129980 (0.001-100 nM; 72 h) inhibits the proliferation of A549 lung cancer cell lines transfected with C4.4A.BAY 1129980 (0.001-100 nM; 72 h) exhibits high and selective efficacy on hC4.4A:A549 cells in vitro.
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