Linker Information
General Information of This Linker
| Linker ID |
LIN0VGFMG
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| Linker Name |
MT-GGFG-AM
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| Linker Type |
Cathepsin-cleavable linker
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| Antibody-Linker Relation |
Cleavable
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| Structure |
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| Formula |
C29H40N6O10
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| Isosmiles |
O=C(NCC(N[C@@H](CC1=CC=CC=C1)C(NCC(NC)=O)=O)=O)CNC(CCOCCOCCOCCN2C(C=CC2=O)=O)=O
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| InChI |
InChI=1S/C29H40N6O10/c1-30-24(37)18-33-29(42)22(17-21-5-3-2-4-6-21)34-26(39)20-32-25(38)19-31-23(36)9-11-43-13-15-45-16-14-44-12-10-35-27(40)7-8-28(35)41/h2-8,22H,9-20H2,1H3,(H,30,37)(H,31,36)(H,32,38)(H,33,42)(H,34,39)/t22-/m0/s1
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| InChIKey |
KNZZGNKBPXMFAO-QFIPXVFZSA-N
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| Pharmaceutical Properties |
Molecule Weight
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632.671
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Polar area
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210.57
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Complexity
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1117.738212
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xlogp Value
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-2.8266
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Heavy Count
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45
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Rot Bonds
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22
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Hbond acc
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10
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Hbond Donor
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5
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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
38354417 T-DL11 [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) |
0.002 nM
|
High HER2 expression (HER2 +++) | ||
| Method Description |
A total of 30,000 SK-BR-3 (HER2-high) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
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| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | > 100 nM | Negative HER2 expression (HER2-) | ||
| Method Description |
A total of 10,000 MDA-MB-468 (HER2-negative) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
38354417 T-DL5 [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) |
0.003 nM
|
High HER2 expression (HER2 +++) | ||
| Method Description |
A total of 30,000 SK-BR-3 (HER2-high) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
|
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| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | > 100 nM | Negative HER2 expression (HER2-) | ||
| Method Description |
A total of 10,000 MDA-MB-468 (HER2-negative) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
38354417 T-DL13 [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) |
0.003 nM
|
High HER2 expression (HER2 +++) | ||
| Method Description |
A total of 30,000 SK-BR-3 (HER2-high) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
|
||||
| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | > 100 nM | Negative HER2 expression (HER2-) | ||
| Method Description |
A total of 10,000 MDA-MB-468 (HER2-negative) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
|
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
38354417 T-DL3 [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) |
0.007 nM
|
High HER2 expression (HER2 +++) | ||
| Method Description |
A total of 30,000 SK-BR-3 (HER2-high) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
|
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| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | > 30 nM | Negative HER2 expression (HER2-) | ||
| Method Description |
A total of 10,000 MDA-MB-468 (HER2-negative) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
38354417 T-DL7 [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) |
0.009 nM
|
High HER2 expression (HER2 +++) | ||
| Method Description |
A total of 30,000 SK-BR-3 (HER2-high) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
|
||||
| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | > 30 nM | Negative HER2 expression (HER2-) | ||
| Method Description |
A total of 10,000 MDA-MB-468 (HER2-negative) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
|
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
38354417 T-DL4 [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) |
0.014 nM
|
High HER2 expression (HER2 +++) | ||
| Method Description |
A total of 30,000 SK-BR-3 (HER2-high) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
|
||||
| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
5 nM
|
Negative HER2 expression (HER2-) | ||
| Method Description |
A total of 10,000 MDA-MB-468 (HER2-negative) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
|
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
38354417 T-DL1 [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) |
0.015 nM
|
High HER2 expression (HER2 +++) | ||
| Method Description |
A total of 30,000 SK-BR-3 (HER2-high) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
|
||||
| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | > 100 nM | Negative HER2 expression (HER2-) | ||
| Method Description |
A total of 10,000 MDA-MB-468 (HER2-negative) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
|
||||
| In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
38354417 T-DL9 [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) |
0.51 nM
|
High HER2 expression (HER2 +++) | ||
| Method Description |
A total of 30,000 SK-BR-3 (HER2-high) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
|
||||
| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | > 30 nM | Negative HER2 expression (HER2-) | ||
| Method Description |
A total of 10,000 MDA-MB-468 (HER2-negative) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
|
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
38354417 T-DL14 [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) |
2.9 nM
|
High HER2 expression (HER2 +++) | ||
| Method Description |
A total of 30,000 SK-BR-3 (HER2-high) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
|
||||
| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | > 30 nM | Negative HER2 expression (HER2-) | ||
| Method Description |
A total of 10,000 MDA-MB-468 (HER2-negative) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
|
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
References