General Information of This Payload
Payload ID
PAY0USQYR
Name
AU2023267043A1 ADC-5 Payload
Synonyms
AU2023267043A1 ADC-5 Payload
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Structure
Formula
C40H69N9O6
Isosmiles
CC([C@H](N(C)C)C(N[C@@H](C(C)C)C(N([C@H]([C@H](OC)CC(N1CCC[C@H]1[C@H](OC)[C@H](C(N[C@H](CN=[N+]=[N-])CC2=CC=C(N)C=C2)=O)C)=O)[C@H](CC)C)C)=O)=O)C
InChI
InChI=1S/C40H69N9O6/c1-13-26(6)36(48(10)40(53)34(24(2)3)45-39(52)35(25(4)5)47(8)9)32(54-11)22-33(50)49-20-14-15-31(49)37(55-12)27(7)38(51)44-30(23-43-46-42)21-28-16-18-29(41)19-17-28/h16-19,24-27,30-32,34-37H,13-15,20-23,41H2,1-12H3,(H,44,51)(H,45,52)/t26-,27+,30-,31-,32+,34-,35-,36-,37+/m0/s1
InChIKey
QIHHTRNUHMRKQK-MNFMTBGBSA-N
Pharmaceutical Properties
Molecule Weight
772.049
Polar area
195.3
Complexity
1365.212769
xlogp Value
4.2537
Heavy Count
55
Rot Bonds
22
Hbond acc
9
Hbond Donor
3
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
anti-FOLR1-151-K-LOCK-D5 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 7 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
77.29%
Method Description
The anti-tumor efficacy of a single dose of 1.5 mg/kg 151-K-Lock-D5 (ADC-5)
In Vivo Model NSCLC cancer PDX model LU-01-1618
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
0.97%
Method Description
The anti-tumor efficacy of a single dose of 1.5 mg/kg 151-K-Lock-D5 (ADC-5)
In Vivo Model IGROV1 tumor xenograft model
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
1.00%
Method Description
The anti-tumor efficacy of a single dose of 1.5 mg/kg 151-K-Lock-D5 (ADC-5)
In Vivo Model IGROV1 tumor xenograft model
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
105.97%
Method Description
The anti-tumor efficacy of a single dose of 1.5 mg/kg 151-K-Lock-D5 (ADC-5)
In Vivo Model NSCLC cancer PDX model LU-01-1618
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
111.94%
Method Description
The anti-tumor efficacy of a single dose of 1.5 mg/kg 151-K-Lock-D5 (ADC-5)
In Vivo Model NSCLC cancer PDX model LU-01-1618
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
116.16%
Method Description
The anti-tumor efficacy of a single dose of 1.5 mg/kg 151-K-Lock-D5 (ADC-5)
In Vivo Model NSCLC cancer PDX model LU-01-1618
Experiment 7 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
116.16%
Method Description
The anti-tumor efficacy of a single dose of 1.5 mg/kg 151-K-Lock-D5 (ADC-5)
In Vivo Model IGROV1 tumor xenograft model
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.55 nM
High IGROV1 expression (IGROV1 +++)
Method Description
IC50 Values (nM) of anti-FOLR1-151-K-LOCK-D5 and their corresponding controls in Human Tumor Cells IGROV1.
In Vitro Model Endometrioid carcinoma of ovary, Ovarian endometrioid adenocarcinoma IGROV1 cells CVCL_1304
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
15 nM
Low SKOV-3 expression ( SKOV-3 +)
Method Description
IC50 Values (nM) of anti-FOLR1-151-K-LOCK-D5 and their corresponding controls in Human Tumor Cells SKOV-3
In Vitro Model Ovarian serous adenocarcinoma SKOV-3 cells CVCL_0532
References
Ref 1 Antibody-drug conjugates comprising an anti-FOLR1 antibody