1404071-37-9

1404071-37-9 structure
1404071-37-9 structure
  • Name: BAY 1135626
  • Chemical Name: BAY 1135626
  • CAS Number: 1404071-37-9
  • Molecular Formula: C55H86N10O11
  • Molecular Weight: 1063.33
  • Catalog: Research Areas Cancer
  • Create Date: 2022-09-11 21:37:06
  • Modify Date: 2024-01-10 01:06:31
  • 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–drug conjugate (ADC), is used to non–small cell lung cancer (NSCLC) research[1].

Name BAY 1135626
Description 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–drug conjugate (ADC), is used to non–small cell lung cancer (NSCLC) research[1].
Related Catalog
In Vitro C4.4A (LYPD3) is a protein expressed in non-small cell lung cancer (NSCLC), with scarcely expressing in normal tissues[1]. BAY 1135626 can be synthesized into BAY 1129980 (C4.4A-ADC), shows a strong anti-proliferative effect on C4.4A expressing cell lines[1]. BAY 1129980 (0.001-100 nM; 72 h) inhibits the proliferation of A549 lung cancer cell lines transfected with C4.4A[1]. BAY 1129980 (0.001-100 nM; 72 h) exhibits high and selective efficacy on hC4.4A:A549 cells in vitro[1]. Cell Cytotoxicity Assay[1] Cell Line: hC4.4A:A549 lung cancer cells Concentration: 0.001-100 nM Incubation Time: 72 hours Result: High potency at subnanomolar range with an IC50 value of 0.05 nM. Resulted remarkable selectivity on hC4.4A:A549 with over 1,000-fold compared with mock:A549 cells. Cell Viability Assay[1] Cell Line: NCI-H292, FaDu, NCI-H322, SCaBER, SCC-4 Concentration: 0.001-100 nM Incubation Time: 72 hours Result: Inhibited cancer cell growth in a dose-dependent manner.
In Vivo BAY 1129980 (1.9-7.5 mg/kg; i.v.; 20 d) inhibits tumor growth in vivo in mouse[1]. 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[1]. Animal Model: C4.4A-positive NCI-H292 NSCLC xenograft mouse model[1] 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[1] 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.
References

[1]. Willuda J, et al. Preclinical Antitumor Efficacy of BAY 1129980-a Novel Auristatin-Based Anti-C4.4A (LYPD3) Antibody-Drug Conjugate for the Treatment of Non-Small Cell Lung Cancer. Mol Cancer Ther. 2017 May. 16(5):893-904.

Molecular Formula C55H86N10O11
Molecular Weight 1063.33
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