Linker Information
General Information of This Linker
| Linker ID |
LIN0VXWAF
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| Linker Name |
CLeavable (Val-Citruline-PEG1) linker
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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 |
C22H38N6O6
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| Isosmiles |
CC([C@H](NCCOCCON)C(N[C@@H](CCCNC(N)=O)C(NC1=CC=C(CO)C=C1)=O)=O)C
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| InChI |
InChI=1S/C22H38N6O6/c1-15(2)19(25-10-11-33-12-13-34-24)21(31)28-18(4-3-9-26-22(23)32)20(30)27-17-7-5-16(14-29)6-8-17/h5-8,15,18-19,25,29H,3-4,9-14,24H2,1-2H3,(H,27,30)(H,28,31)(H3,23,26,32)/t18-,19-/m0/s1
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| InChIKey |
PQDMWBFPMXUJKZ-OALUTQOASA-N
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| Pharmaceutical Properties |
Molecule Weight
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482.582
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Polar area
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190.06
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Complexity
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702.0587879
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xlogp Value
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-0.4282
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Heavy Count
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34
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Rot Bonds
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17
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Hbond acc
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8
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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 ADC13 [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) |
0.047 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 ADC8 [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) |
0.051 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 ADC3 [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) |
0.066 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 | ||