Linker Information
General Information of This Linker
| Linker ID |
LIN0RBZIU
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| Linker Name |
US20250000993A1 ADC Linker
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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 |
C13H16N2O9S
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| Isosmiles |
O=C(O)CN1C(=O)[C@@H](N2C(=O)C=CC2=O)C[C@H]1COCCS(=O)(=O)O
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| PubChem CID | ||||||
| InChI |
InChI=1S/C13H16N2O9S/c16-10-1-2-11(17)15(10)9-5-8(7-24-3-4-25(21,22)23)14(13(9)20)6-12(18)19/h1-2,8-9H,3-7H2,(H,18,19)(H,21,22,23)/t8-,9-/m0/s1
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| InChIKey |
YHTHBPJQKAVIGL-IUCAKERBSA-N
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| Pharmaceutical Properties |
Molecule Weight
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376.343
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Polar area
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158.59
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Complexity
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674.3203425
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xlogp Value
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-2.1301
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Heavy Count
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25
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Rot Bonds
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8
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Hbond acc
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7
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Hbond Donor
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2
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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
Anti-Human CD33 BETd ADCs [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | < 0.005 nM | |||
| Method Description |
Proliferation of AML cell lines in AML2 following treatment with ADCs, EC50 in mAb1-LD2
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| In Vitro Model | Adult acute myeloid leukemia, Acute myeloid leukemia with t(6;11)(q27;q23) KMT2A-MLLT4, Acute myeloid leukemia | AML2 cells | CVCL_1619 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.005 nM
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| Method Description |
Proliferation of AML cell lines in MOLM13 following treatment with ADCs, EC50 in mAb1-LD2
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| In Vitro Model | Adult acute myeloid leukemia | MOLM-13 cells | CVCL_2119 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.005 nM
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| Method Description |
Proliferation of AML cell lines in MV411 following treatment with ADCs, EC50 in mAb1-LD2
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| In Vitro Model | Childhood acute monocytic leukemia | MV4-11 cells | CVCL_0064 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | < 0.005 nM | |||
| Method Description |
Proliferation of AML cell lines in AML2 following treatment with ADCs, EC50 in mAb1-LD3
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| In Vitro Model | Adult acute myeloid leukemia, Acute myeloid leukemia with t(6;11)(q27;q23) KMT2A-MLLT4, Acute myeloid leukemia | AML2 cells | CVCL_1619 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.005 nM
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| Method Description |
Proliferation of AML cell lines in MOLM13 following treatment with ADCs, EC50 in mAb1-LD3
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| In Vitro Model | Adult acute myeloid leukemia | MOLM-13 cells | CVCL_2119 | ||
| Experiment 6 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | < 0.005 nM | |||
| Method Description |
Proliferation of AML cell lines in MV411 following treatment with ADCs, EC50 in mAb1-LD3
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| In Vitro Model | Childhood acute monocytic leukemia | MV4-11 cells | CVCL_0064 | ||
| Experiment 7 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.039 nM
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| Method Description |
Proliferation of AML cell lines in THP1 following treatment with ADCs, EC50 in mAb1-LD2
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| In Vitro Model | Acute monoblastic/monocytic leukemia, Childhood acute monocytic leukemia | THP1 cells | CVCL_0006 | ||
| Experiment 8 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.073 nM
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| Method Description |
Proliferation of AML cell lines in THP1 following treatment with ADCs, EC50 in mAb1-LD3
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| In Vitro Model | Acute monoblastic/monocytic leukemia, Childhood acute monocytic leukemia | THP1 cells | CVCL_0006 | ||
| Experiment 9 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
9.29 nM
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| Method Description |
Proliferation of AML cell lines in MV411 following treatment with ADCs, EC50 in mAb3-LD3
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| In Vitro Model | Childhood acute monocytic leukemia | MV4-11 cells | CVCL_0064 | ||
| Experiment 10 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
12.29 nM
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| Method Description |
Proliferation of AML cell lines in AML2 following treatment with ADCs, EC50 in mAb3-LD3
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| In Vitro Model | Adult acute myeloid leukemia, Acute myeloid leukemia with t(6;11)(q27;q23) KMT2A-MLLT4, Acute myeloid leukemia | AML2 cells | CVCL_1619 | ||
| Experiment 11 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
14.38 nM
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| Method Description |
Proliferation of AML cell lines in MOLM13 following treatment with ADCs, EC50 in mAb3-LD3
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| In Vitro Model | Adult acute myeloid leukemia | MOLM-13 cells | CVCL_2119 | ||
| Experiment 12 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
20.27 nM
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| Method Description |
Proliferation of AML cell lines in THP1 following treatment with ADCs, EC50 in mAb3-LD3
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| In Vitro Model | Acute monoblastic/monocytic leukemia, Childhood acute monocytic leukemia | THP1 cells | CVCL_0006 | ||