Linker Information
General Information of This Linker
| Linker ID |
LIN0XCJLG
|
|||||
|---|---|---|---|---|---|---|
| Linker Name |
US20240269308A1 aHer2- (AL7-LP5D)n Linker
|
|||||
| Linker Type |
Unclear
|
|||||
| Antibody-Linker Relation |
Unclear
|
|||||
| Structure |
|
|||||
| Formula |
C44H69N7O14
|
|||||
| Isosmiles |
CC([C@@H](C(N[C@@H](CCCNC(N)=O)C(NC1=CC=C(CO)C=C1)=O)=O)NC([C@@H](NC(CCOCCOCCOCCOCCNC(COC2CCCCCC#C2)=O)=O)CCC(O)=O)=O)C
|
|||||
| InChI |
InChI=1S/C44H69N7O14/c1-31(2)40(43(59)50-35(11-8-19-47-44(45)60)41(57)48-33-14-12-32(29-52)13-15-33)51-42(58)36(16-17-39(55)56)49-37(53)18-21-61-23-25-63-27-28-64-26-24-62-22-20-46-38(54)30-65-34-9-6-4-3-5-7-10-34/h12-15,31,34-36,40,52H,3-6,8-9,11,16-30H2,1-2H3,(H,46,54)(H,48,57)(H,49,53)(H,50,59)(H,51,58)(H,55,56)(H3,45,47,60)/t34?,35-,36-,40-/m0/s1
|
|||||
| InChIKey |
QHNAPHNLMJPIBE-NUUHXFNHSA-N
|
|||||
| Pharmaceutical Properties |
Molecule Weight
|
920.071
|
Polar area
|
304.3
|
||
|
Complexity
|
1592.550279
|
xlogp Value
|
0.4665
|
|||
|
Heavy Count
|
65
|
Rot Bonds
|
34
|
|||
|
Hbond acc
|
13
|
Hbond Donor
|
9
|
|||
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
aHer2- (AL7-LP5D)n [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.139 nM
|
High HER2 expression (HER2 +++) | ||
| Method Description |
The cell line used in the anti-proliferation assays was SK-BR-3, a human breast, adenocarcinoma (pleural effusion) cell line; The cells were grown in McCoy's 5a Medium+10% FBS. To run the assay, the cells (80 ul, 1000 cells) were added to each well in a 96-well plate and incubated for 24 hours at 37°C. with CO,. Next, the cells were treated with test compounds (20 ul) at various concentrations in appropriate cell culture medium (total volume, 0.1 mL). The control wells contain cells and the medium but lack the test compounds. The plates were incubated for 144
hours at 37°C. with CO,. CTG reagent was then added to the wells (100 il). After the plates were shaken for 10 min and then incubated for 10 min at room temperature, paste the clear bottom with white back seal and record luminescence with Envision. The inhibition % was calculated according to the following equation: inhibition %=[1- (assay-blank)/ (control-blank)|x100.
Click to Show/Hide
|
||||
| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
FeID1- (AL7-LP5D)n [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
88.2 nM
|
Low ID1 expression (ID1+) | ||
| Method Description |
The cell line used in the anti-proliferation assays was SK-BR-3, a human breast, adenocarcinoma (pleural effusion) cell line; The cells were grown in McCoy's 5a Medium+10% FBS. To run the assay, the cells (80 ul, 1000 cells) were added to each well in a 96-well plate and incubated for 24 hours at 37°C. with CO,. Next, the cells were treated with test compounds (20 ul) at various concentrations in appropriate cell culture medium (total volume, 0.1 mL). The control wells contain cells and the medium but lack the test compounds. The plates were incubated for 144
hours at 37°C. with CO,. CTG reagent was then added to the wells (100 il). After the plates were shaken for 10 min and then incubated for 10 min at room temperature, paste the clear bottom with white back seal and record luminescence with Envision. The inhibition % was calculated according to the following equation: inhibition %=[1- (assay-blank)/ (control-blank)|x100.
Click to Show/Hide
|
||||
| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
References