Linker Information
General Information of This Linker
| Linker ID |
LIN0KIDPE
|
|||||
|---|---|---|---|---|---|---|
| Linker Name |
AU2023267043A1 ADC-5 Linker
|
|||||
| Linker Type |
Cathepsin-cleavable linker
|
|||||
| Antibody-Linker Relation |
Cleavable
|
|||||
| Structure |
|
|||||
| Formula |
C23H43N6O6
|
|||||
| Isosmiles |
CNC(C1CCN(CC1)C(CCC(N[C@@H](C(C)C)C(N[C@H](C(C)=O)CCCNCN)=O)=O)=O)=O.[OH]
|
|||||
| InChI |
InChI=1S/C23H42N6O5.HO/c1-15(2)21(23(34)27-18(16(3)30)6-5-11-26-14-24)28-19(31)7-8-20(32)29-12-9-17(10-13-29)22(33)25-4;/h15,17-18,21,26H,5-14,24H2,1-4H3,(H,25,33)(H,27,34)(H,28,31);1H/t18-,21-;/m0./s1
|
|||||
| InChIKey |
COWYQCBDXRLLKO-ZXRBMNSTSA-N
|
|||||
| Pharmaceutical Properties |
Molecule Weight
|
499.633
|
Polar area
|
192.73
|
||
|
Complexity
|
664.1518798
|
xlogp Value
|
-0.925
|
|||
|
Heavy Count
|
35
|
Rot Bonds
|
14
|
|||
|
Hbond acc
|
7
|
Hbond Donor
|
6
|
|||
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
anti-FOLR1-151-K-LOCK-D5 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
| 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
| 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 | ||