Linker Information
General Information of This Linker
| Linker ID |
LIN0RTLEV
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| Linker Name |
WO2025019776A2, ADC 22-2, 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 |
C44H65N9O18S
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| Isosmiles |
CNN(CC1=CC(C=CC=N2)=C2N1CCC(N[C@@H](CS(=O)(O)=O)C(NCCOCCOCCC(N[C@H](C(N[C@@H](C)C(NC3=C(O[C@H]4[C@H](O)[C@@H](O)[C@H](O)[C@H](C(O)=O)O4)C=C(C=C3)CO)=O)=O)C(C)C)=O)=O)=O)C
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| InChI |
InChI=1S/C44H65N9O18S/c1-24(2)34(42(62)48-25(3)40(60)50-29-9-8-26(22-54)19-31(29)70-44-37(59)35(57)36(58)38(71-44)43(63)64)51-33(56)11-15-68-17-18-69-16-13-47-41(61)30(23-72(65,66)67)49-32(55)10-14-53-28(21-52(5)45-4)20-27-7-6-12-46-39(27)53/h6-9,12,19-20,24-25,30,34-38,44-45,54,57-59H,10-11,13-18,21-23H2,1-5H3,(H,47,61)(H,48,62)(H,49,55)(H,50,60)(H,51,56)(H,63,64)(H,65,66,67)/t25-,30-,34-,35-,36-,37+,38+,44+/m0/s1
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| InChIKey |
PMIAQAZSCQRYTC-TVLGZQFRSA-N
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| Pharmaceutical Properties |
Molecule Weight
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1040.116
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Polar area
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388.1
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Complexity
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2341.806261
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xlogp Value
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-3.0478
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Heavy Count
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72
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Rot Bonds
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29
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Hbond acc
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20
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Hbond Donor
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12
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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
wO2025019776A2ADC 33-2 [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) |
37.50%
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Positive IL13Ra2 expression (IL13Ra2+++/++) | ||
| Method Description |
Each female BALB/c Nude mouse was inoculated subcutaneously in the right upper flank region with 0.5x10 6of SK-MES-1 tumor cells (a non-small cell lung cancer (NSCLC)cell line having an IL13Ra2 copy number of about 4x104)in 0.1 mL of PBS for tumor development.When the mean tumor size reached about 80-150 mm 3,mice were randomized into respective treatment groups (8 mice per group)and received intravenous injections of PBS vehicle or a single dose of the tested ADC 33-2 at 1 mg/kg on Day 1. The end of the study was day 44.
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| In Vivo Model | CDX Model-SK-MES-1 | ||||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) |
55%
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Positive IL13Ra2 expression (IL13Ra2+++/++) | ||
| Method Description |
Each female BALB/c Nude mouse was inoculated subcutaneously in the right upper flank region with 0.5x10 6of SK-MES-1 tumor cells (a non-small cell lung cancer (NSCLC)cell line having an IL13Ra2 copy number of about 4x104)in 0.1 mL of PBS for tumor development.When the mean tumor size reached about 80-150 mm 3,mice were randomized into respective treatment groups (8 mice per group)and received intravenous injections of PBS vehicle or a single dose of the tested ADC 33-2 at 3 mg/kg on Day 1. The end of the study was day 44.
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| In Vivo Model | CDX Model-SK-MES-1 | ||||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) |
82.20%
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Positive IL13Ra2 expression (IL13Ra2+++/++) | ||
| Method Description |
Each female BALB/c Nude mouse was inoculated subcutaneously in the right upper flank region with 0.5x10 6of SK-MES-1 tumor cells (a non-small cell lung cancer (NSCLC)cell line having an IL13Ra2 copy number of about 4x104)in 0.1 mL of PBS for tumor development.When the mean tumor size reached about 80-150 mm 3,mice were randomized into respective treatment groups (8 mice per group)and received intravenous injections of PBS vehicle or a single dose of the tested ADC 33-2 at 6 mg/kg on Day 1. The end of the study was day 44.
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| In Vivo Model | CDX Model-SK-MES-1 | ||||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) |
88.60%
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Positive IL13Ra2 expression (IL13Ra2+++/++) | ||
| Method Description |
Each female BALB/c Nude mouse was inoculated subcutaneously in the right upper/lower flank region with 1x10 7of H2228 tumor cells (an NSCLC cell line having an IL13Ra2 copy number of about 2,000)in 0.1 mL of PBS mixed with MATRIGELR (1:1)for tumor development.When the mean tumor size reached about 80-150 mm 3,mice were randomized into respective treatment groups (10 mice per group)and received intravenous injections of vehicle or a single dose of the tested ADCs at 10 mg/kg on Day 1. Body weights and tumor volumes were measured twice per week until the end of the study (Day 48).
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| In Vivo Model | CDX Model-H2228 | ||||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) |
100%
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Positive IL13Ra2 expression (IL13Ra2+++/++) | ||
| Method Description |
Each female BALB/c Nude mouse was inoculated subcutaneously in the right upper flank region with 0.5x10 6of SK-MES-1 tumor cells (a non-small cell lung cancer (NSCLC)cell line having an IL13Ra2 copy number of about 4x104)in 0.1 mL of PBS for tumor development.When the mean tumor size reached about 80-150 mm 3,mice were randomized into respective treatment groups (8 mice per group)and received intravenous injections of PBS vehicle or a single dose of the tested ADC 33-2 at 10 mg/kg on Day 1. The end of the study was day 44.
Click to Show/Hide
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| In Vivo Model | CDX Model-SK-MES-1 | ||||
| Experiment 6 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) |
101.10%
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Positive IL13Ra2 expression (IL13Ra2+++/++) | ||
| Method Description |
Each female BALB/c Nude mouse was inoculated subcutaneously in the right upper flank region with 0.5x10 6of SK-MES-1 tumor cells (a non-small cell lung cancer (NSCLC)cell line having an IL13Ra2 copy number of about 4x104)in 0.1 mL of PBS for tumor development.When the mean tumor size reached about 80-150 mm 3,mice were randomized into respective treatment groups (10 mice per group)and received intravenous injections of PBS vehicle or a single dose of the tested ADCs at 10 mg/kg on Day 1. The end of the study was day 49.
Click to Show/Hide
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| In Vivo Model | CDX Model-SK-MES-1 | ||||
| Experiment 7 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) |
111%
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Positive IL13Ra2 expression (IL13Ra2+++/++) | ||
| Method Description |
Each female NOD.Cg-Prkdcscid II2rgmIVst/Vst (NPG)mouse was inoculated subcutaneously in the right upper flank region with 1x10 7of H1792 tumor cells (an NSCLC cell line having an IL13Ra2 copy number of about 47000)in 0.1 mL of PBS mixed with MATRIGELR (1:1)for tumor development.When the mean tumor size reached about 80-150 mm 3,mice were randomized into respective treatment groups (10 mice per group)and received intravenous injections of vehicle or a single dose of the tested ADCs at 10 mg/kg on Day 1. Body weights and tumor volumes were measured twice per week until the end of the study (Day 57).
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| In Vivo Model | CDX Model-H1792 | ||||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.01 nM
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High hIL13Ra2 expression (hIL13Ra2 +++) | ||
| Method Description |
The cytotoxic activity of ADC 33-2 was determined against cancer cell lines A375.FITC and anti-Hen egg-white lysozyme isotype control antibody (HEWL)conjugated to the same linker payloads.
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| In Vitro Model | Amelanotic melanoma | A375 cells | CVCL_0132 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.02-0.03 nM
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Positive hIL13Ra2 expression (hIL13Ra2+++/++) | ||
| Method Description |
The cytotoxic activity of ADC 33-2 was determined against cancer cell lines H1792.FITC and anti-Hen egg-white lysozyme isotype control antibody (HEWL)conjugated to the same linker payloads.
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| In Vitro Model | Lung adenocarcinoma | H1792 cells | CVCL_1495 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.04-0.08 nM
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Positive hIL13Ra2 expression (hIL13Ra2+++/++) | ||
| Method Description |
The cytotoxic activity of ADC 33-2 was determined against cancer cell lines H2228.FITC and anti-Hen egg-white lysozyme isotype control antibody (HEWL)conjugated to the same linker payloads.
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| In Vitro Model | Lung adenocarcinoma | H2228 cells | CVCL_1543 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
3-63 nM
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Positive hIL13Ra2 expression (hIL13Ra2+++/++) | ||
| Method Description |
The cytotoxic activity of ADC 33-2 was determined against cancer cell lines SK-MES-1.FITC and anti-Hen egg-white lysozyme isotype control antibody (HEWL)conjugated to the same linker payloads.
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| In Vitro Model | Lung squamous cell carcinoma | SK-MES-1 cells | CVCL_0630 | ||
wO2025019776A2ADC 22-2 [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) |
81.20%
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Positive IL13Ra2 expression (IL13Ra2+++/++) | ||
| Method Description |
Each female BALB/c Nude mouse was inoculated subcutaneously in the right upper flank region with 0.5x10 6of SK-MES-1 tumor cells (a non-small cell lung cancer (NSCLC)cell line having an IL13Ra2 copy number of about 4x104)in 0.1 mL of PBS for tumor development.When the mean tumor size reached about 80-150 mm 3,mice were randomized into respective treatment groups (10 mice per group)and received intravenous injections of PBS vehicle or a single dose of the tested ADCs at 10 mg/kg on Day 1. The end of the study was day 49.
Click to Show/Hide
|
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| In Vivo Model | CDX Model-SK-MES-1 | ||||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) |
82.30%
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Positive IL13Ra2 expression (IL13Ra2+++/++) | ||
| Method Description |
Each female BALB/c Nude mouse was inoculated subcutaneously in the right upper/lower flank region with 1x10 7of H2228 tumor cells (an NSCLC cell line having an IL13Ra2 copy number of about 2,000)in 0.1 mL of PBS mixed with MATRIGELR (1:1)for tumor development.When the mean tumor size reached about 80-150 mm 3,mice were randomized into respective treatment groups (10 mice per group)and received intravenous injections of vehicle or a single dose of the tested ADCs at 10 mg/kg on Day 1. Body weights and tumor volumes were measured twice per week until the end of the study (Day 48).
Click to Show/Hide
|
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| In Vivo Model | CDX Model-H2228 | ||||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.01 nM
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High hIL13Ra2 expression (hIL13Ra2 +++) | ||
| Method Description |
The cytotoxic activity of ADC 22-2 was determined against cancer cell lines A375.FITC and anti-Hen egg-white lysozyme isotype control antibody (HEWL)conjugated to the same linker payloads.
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| In Vitro Model | Amelanotic melanoma | A375 cells | CVCL_0132 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.02-0.03 nM
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Positive hIL13Ra2 expression (hIL13Ra2+++/++) | ||
| Method Description |
The cytotoxic activity of ADC 22-2 was determined against cancer cell lines H1792.FITC and anti-Hen egg-white lysozyme isotype control antibody (HEWL)conjugated to the same linker payloads.
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| In Vitro Model | Lung adenocarcinoma | H1792 cells | CVCL_1495 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.04-0.08 nM
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Positive hIL13Ra2 expression (hIL13Ra2+++/++) | ||
| Method Description |
The cytotoxic activity of ADC 22-2 was determined against cancer cell lines H2228.FITC and anti-Hen egg-white lysozyme isotype control antibody (HEWL)conjugated to the same linker payloads.
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| In Vitro Model | Lung adenocarcinoma | H2228 cells | CVCL_1543 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
3-63 nM
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Positive hIL13Ra2 expression (hIL13Ra2+++/++) | ||
| Method Description |
The cytotoxic activity of ADC 22-2 was determined against cancer cell lines SK-MES-1.FITC and anti-Hen egg-white lysozyme isotype control antibody (HEWL)conjugated to the same linker payloads.
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| In Vitro Model | Lung squamous cell carcinoma | SK-MES-1 cells | CVCL_0630 | ||
wO2025019776A2ADC 52-2 [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) |
0.01 nM
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High hIL13Ra2 expression (hIL13Ra2 +++) | ||
| Method Description |
The cytotoxic activity of ADC 52-2 was determined against cancer cell lines A375.FITC and anti-Hen egg-white lysozyme isotype control antibody (HEWL)conjugated to the same linker payloads.
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| In Vitro Model | Amelanotic melanoma | A375 cells | CVCL_0132 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.02-0.03 nM
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Positive hIL13Ra2 expression (hIL13Ra2+++/++) | ||
| Method Description |
The cytotoxic activity of ADC 52-2 was determined against cancer cell lines H1792.FITC and anti-Hen egg-white lysozyme isotype control antibody (HEWL)conjugated to the same linker payloads.
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| In Vitro Model | Lung adenocarcinoma | H1792 cells | CVCL_1495 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.04-0.08 nM
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Positive hIL13Ra2 expression (hIL13Ra2+++/++) | ||
| Method Description |
The cytotoxic activity of ADC 52-2 was determined against cancer cell lines H2228.FITC and anti-Hen egg-white lysozyme isotype control antibody (HEWL)conjugated to the same linker payloads.
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| In Vitro Model | Lung adenocarcinoma | H2228 cells | CVCL_1543 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
3-63 nM
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Positive hIL13Ra2 expression (hIL13Ra2+++/++) | ||
| Method Description |
The cytotoxic activity of ADC 52-2 was determined against cancer cell lines SK-MES-1.FITC and anti-Hen egg-white lysozyme isotype control antibody (HEWL)conjugated to the same linker payloads.
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| In Vitro Model | Lung squamous cell carcinoma | SK-MES-1 cells | CVCL_0630 | ||