Linker Information
General Information of This Linker
| Linker ID |
LIN0EDPXW
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| Linker Name |
Mcc-hydrazide
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| Linker Type |
Flexible dual-reactive (thiol) linker
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| Antibody-Linker Relation |
Uncleavable
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| Structure |
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| Formula |
C12H17N3O3
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| Isosmiles |
NNC(=O)C1CCC(CN2C(=O)C=CC2=O)CC1
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| InChI |
InChI=1S/C12H17N3O3/c13-14-12(18)9-3-1-8(2-4-9)7-15-10(16)5-6-11(15)17/h5-6,8-9H,1-4,7,13H2,(H,14,18)
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| InChIKey |
BYLZUECTWAELHO-UHFFFAOYSA-N
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| Pharmaceutical Properties |
Molecule Weight
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251.286
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Polar area
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92.5
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Complexity
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18
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xlogp Value
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-0.2923
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Heavy Count
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18
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Rot Bonds
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3
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Hbond acc
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4
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Hbond Donor
|
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
Milatuzumab doxorubicin [Terminated in phase 2]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.80 uM
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Positive CD74 expression (CD74+++/++) | ||
| Method Description |
Briefly, cells were placed in 96-well plates (2 x105 per well) and subsequently incubated with serial dilutions of IMMU-110,naked hLL1,nonspecific negative control mAb-drug conjugate (hRS7-doxorubicin),or nonspecific mAb (hRS7) on ice for 1.5 hours. 4-hour IC50 values of IMMU-110,hRS7-doxorubicin,and free doxorubicin against the multiple myeloma cell line (MC/CAR) and other CD74-positive non-Hodgkin's lymphoma cell lines (Daudi and Raji).
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| In Vitro Model | EBV-related Burkitt lymphoma | Raji cells | CVCL_0511 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.90 uM
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Positive CD74 expression (CD74+++/++) | ||
| Method Description |
Briefly, cells were placed in 96-well plates (2 x105 per well) and subsequently incubated with serial dilutions of IMMU-110,naked hLL1,nonspecific negative control mAb-drug conjugate (hRS7-doxorubicin),or nonspecific mAb (hRS7) on ice for 1.5 hours. 4-hour IC50 values of IMMU-110,hRS7-doxorubicin,and free doxorubicin against the multiple myeloma cell line (MC/CAR) and other CD74-positive non-Hodgkin's lymphoma cell lines (Daudi and Raji).
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| In Vitro Model | Normal | MC/CAR cells | CVCL_1397 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.50 uM
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Positive CD74 expression (CD74+++/++) | ||
| Method Description |
Briefly, cells were placed in 96-well plates (2 x105 per well) and subsequently incubated with serial dilutions of IMMU-110,naked hLL1,nonspecific negative control mAb-drug conjugate (hRS7-doxorubicin),or nonspecific mAb (hRS7) on ice for 1.5 hours. 4-hour IC50 values of IMMU-110,hRS7-doxorubicin,and free doxorubicin against the multiple myeloma cell line (MC/CAR) and other CD74-positive non-Hodgkin's lymphoma cell lines (Daudi and Raji).
Click to Show/Hide
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| In Vitro Model | Burkitt lymphoma | Daudi cells | CVCL_0008 | ||
References
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