Linker Information
General Information of This Linker
| Linker ID |
LIN0BZBLZ
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| Linker Name |
Short Cleavable (Valine-Citruline-Acetyl)
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| Linker Type |
Unclear
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| Antibody-Linker Relation |
Unclear
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| Structure |
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| Formula |
C20H32N6O6
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| Isosmiles |
CC([C@H](NC(CON)=O)C(N[C@@H](CCCNC(N)=O)C(NC1=CC=C(C=C1)CO)=O)=O)C
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| InChI |
InChI=1S/C20H32N6O6/c1-12(2)17(26-16(28)11-32-22)19(30)25-15(4-3-9-23-20(21)31)18(29)24-14-7-5-13(10-27)6-8-14/h5-8,12,15,17,27H,3-4,9-11,22H2,1-2H3,(H,24,29)(H,25,30)(H,26,28)(H3,21,23,31)/t15-,17-/m0/s1
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| InChIKey |
MPIYPINVBXWLJF-RDJZCZTQSA-N
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| Pharmaceutical Properties |
Molecule Weight
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452.512
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Polar area
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197.9
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Complexity
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727.8067451
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xlogp Value
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-0.9182
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Heavy Count
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32
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Rot Bonds
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13
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Hbond acc
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7
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Hbond Donor
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7
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Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
EP4461318A2 anti-PSMA ADC14 [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) |
0.049 nM
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High FOLH1 expression (FOLH1 +++) | ||
| Method Description |
In Vitro Potency Studies - In vitro potency of anti-PSMA ADCs is determined using a metastatic castration-resistant prostate cancer (mCRPC) representative cell-line, C4-2. The cell culture is incubated with antibody drug conjugates for 96 hours at 37C. Cell viability is analyzed using Cell Titer GlO (Promega, USA). Anti-proliferative activity is represented by potency, ICso, the concentration at which 50% of the maximum activity is achieved and cell killing, and Emax, the maximum level of growth inhibition. Table 5 summarizes the cell killing and in vitro potency of the anti-PSMA ADCs.
Click to Show/Hide
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| In Vitro Model | Prostate carcinoma | C4-2 cells | CVCL_4782 | ||
EP4461318A2 anti-PSMA ADC9 [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) |
0.053 nM
|
High FOLH1 expression (FOLH1 +++) | ||
| Method Description |
In Vitro Potency Studies - In vitro potency of anti-PSMA ADCs is determined using a metastatic castration-resistant prostate cancer (mCRPC) representative cell-line, C4-2. The cell culture is incubated with antibody drug conjugates for 96 hours at 37C. Cell viability is analyzed using Cell Titer GlO (Promega, USA). Anti-proliferative activity is represented by potency, ICso, the concentration at which 50% of the maximum activity is achieved and cell killing, and Emax, the maximum level of growth inhibition. Table 5 summarizes the cell killing and in vitro potency of the anti-PSMA ADCs.
Click to Show/Hide
|
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| In Vitro Model | Prostate carcinoma | C4-2 cells | CVCL_4782 | ||
EP4461318A2 anti-PSMA ADC4 [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) |
0.064 nM
|
High FOLH1 expression (FOLH1 +++) | ||
| Method Description |
In Vitro Potency Studies - In vitro potency of anti-PSMA ADCs is determined using a metastatic castration-resistant prostate cancer (mCRPC) representative cell-line, C4-2. The cell culture is incubated with antibody drug conjugates for 96 hours at 37C. Cell viability is analyzed using Cell Titer GlO (Promega, USA). Anti-proliferative activity is represented by potency, ICso, the concentration at which 50% of the maximum activity is achieved and cell killing, and Emax, the maximum level of growth inhibition. Table 5 summarizes the cell killing and in vitro potency of the anti-PSMA ADCs.
Click to Show/Hide
|
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| In Vitro Model | Prostate carcinoma | C4-2 cells | CVCL_4782 | ||
EP4461318A2 anti-PSMA ADC15 [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) |
0.425 nM
|
High FOLH1 expression (FOLH1 +++) | ||
| Method Description |
In Vitro Potency Studies - In vitro potency of anti-PSMA ADCs is determined using a metastatic castration-resistant prostate cancer (mCRPC) representative cell-line, C4-2. The cell culture is incubated with antibody drug conjugates for 96 hours at 37C. Cell viability is analyzed using Cell Titer GlO (Promega, USA). Anti-proliferative activity is represented by potency, ICso, the concentration at which 50% of the maximum activity is achieved and cell killing, and Emax, the maximum level of growth inhibition. Table 5 summarizes the cell killing and in vitro potency of the anti-PSMA ADCs.
Click to Show/Hide
|
||||
| In Vitro Model | Prostate carcinoma | C4-2 cells | CVCL_4782 | ||
EP4461318A2 anti-PSMA ADC10 [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) |
0.52 nM
|
High FOLH1 expression (FOLH1 +++) | ||
| Method Description |
In Vitro Potency Studies - In vitro potency of anti-PSMA ADCs is determined using a metastatic castration-resistant prostate cancer (mCRPC) representative cell-line, C4-2. The cell culture is incubated with antibody drug conjugates for 96 hours at 37C. Cell viability is analyzed using Cell Titer GlO (Promega, USA). Anti-proliferative activity is represented by potency, ICso, the concentration at which 50% of the maximum activity is achieved and cell killing, and Emax, the maximum level of growth inhibition. Table 5 summarizes the cell killing and in vitro potency of the anti-PSMA ADCs.
Click to Show/Hide
|
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| In Vitro Model | Prostate carcinoma | C4-2 cells | CVCL_4782 | ||
EP4461318A2 anti-PSMA ADC5 [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) |
0.542 nM
|
High FOLH1 expression (FOLH1 +++) | ||
| Method Description |
In Vitro Potency Studies - In vitro potency of anti-PSMA ADCs is determined using a metastatic castration-resistant prostate cancer (mCRPC) representative cell-line, C4-2. The cell culture is incubated with antibody drug conjugates for 96 hours at 37C. Cell viability is analyzed using Cell Titer GlO (Promega, USA). Anti-proliferative activity is represented by potency, ICso, the concentration at which 50% of the maximum activity is achieved and cell killing, and Emax, the maximum level of growth inhibition. Table 5 summarizes the cell killing and in vitro potency of the anti-PSMA ADCs.
Click to Show/Hide
|
||||
| In Vitro Model | Prostate carcinoma | C4-2 cells | CVCL_4782 | ||