Linker Information
General Information of This Linker
| Linker ID |
LIN0LUYHB
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| Linker Name |
Drug linker PB038
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| Linker Type |
Cathepsin-cleavable linker
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| Antibody-Linker Relation |
Cleavable
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| Formula |
C73H127N9O31
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| Isosmiles |
CC([C@H](NC([C@@H](NC(CCCCCN1C(C=CC1=O)=O)=O)CCCCNC(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCN(C[C@@H]([C@@H](O)[C@H](O)[C@H](O)CO)O)C[C@H](O)[C@@H](O)C([C@H](O)CO)=O)=O)=O)C(N[C@@H](CCCNC(N)=O)C(NC2=CC=C(C=C2)CO)=O)=O)C
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| InChI |
InChI=1S/C73H127N9O31/c1-52(2)65(72(100)79-56(10-8-20-76-73(74)101)70(98)77-54-14-12-53(49-83)13-15-54)80-71(99)55(78-62(91)11-4-3-7-21-82-63(92)16-17-64(82)93)9-5-6-19-75-61(90)18-23-102-25-27-104-29-31-106-33-35-108-37-39-110-41-43-112-45-46-113-44-42-111-40-38-109-36-34-107-32-30-105-28-26-103-24-22-81(47-57(86)66(94)68(96)59(88)50-84)48-58(87)67(95)69(97)60(89)51-85/h12-17,52,55-60,65-68,83-89,94-96H,3-11,18-51H2,1-2H3,(H,75,90)(H,77,98)(H,78,91)(H,79,100)(H,80,99)(H3,74,76,101)/t55-,56-,57-,58-,59+,60+,65-,66+,67+,68+/m0/s1
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| InChIKey |
SHQXXHAOXJCACX-GFCQNUDWSA-N
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| Pharmaceutical Properties |
Molecule Weight
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1626.851
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Polar area
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571.37
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Complexity
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2617.103511
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xlogp Value
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-5.5805
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Heavy Count
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113
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Rot Bonds
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75
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Hbond acc
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32
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Hbond Donor
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17
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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
WO2024092067A1 ADC 2E7-LD038 (PA038) [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) |
36 nM
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Moderate CD70 expression (CD70++) | ||
| Method Description |
Cell Raji were cultured in CO2, thermostatic incubator at 37°C with 5% CO2, in standard conditions. Cells were sub-cultured every 1-2 days, digested with 0.25% trypsin and passaged with a suitable density. When the cells were in the logarithmic growth phase and the amount meeting the assay's demand, cells were collectedand plated onto 96-well solid white flat bottom plates for assay. One day later test articles 2E7-LD038 conjugate ranging from 2 uM to 0.1nM, or extecan ranging from 20 uM to 0.03 nM were added to the cells. Plates were then incubated at 37°C for 96h. Cell Titer Glo (CTG) (40 ul per well) was subsequently added to the plates. Luciferase reading was collected 5min after and analyzed by Microplatereaders. All readings were normalized as percentage of viable cells in the untreated control wells and theICso yalues were calculated by Prism software.
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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 (lC50) |
37 nM
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| Method Description |
Cell Caki-1 were cultured in CO2, thermostatic incubator at 37°C with 5% CO2, in standard conditions. Cells were sub-cultured every 1-2 days, digested with 0.25% trypsin and passaged with a suitable density. When the cells were in the logarithmic growth phase and the amount meeting the assay's demand, cells were collectedand plated onto 96-well solid white flat bottom plates for assay. One day later test articles 2E7-LD038 conjugate ranging from 2 uM to 0.1nM, or extecan ranging from 20 uM to 0.03 nM were added to the cells. Plates were then incubated at 37°C for 96h. Cell Titer Glo (CTG) (40 ul per well) was subsequently added to the plates. Luciferase reading was collected 5min after and analyzed by Microplatereaders. All readings were normalized as percentage of viable cells in the untreated control wells and theICso yalues were calculated by Prism software.
Click to Show/Hide
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| In Vitro Model | Clear cell renal cell carcinoma | Caki-1 cells | CVCL_0234 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
292 nM
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| Method Description |
Cell 786-O were cultured in CO2, thermostatic incubator at 37°C with 5% CO2, in standard conditions. Cells were sub-cultured every 1-2 days, digested with 0.25% trypsin and passaged with a suitable density. When the cells were in the logarithmic growth phase and the amount meeting the assay's demand, cells were collectedand plated onto 96-well solid white flat bottom plates for assay. One day later test articles 2E7-LD038 conjugate ranging from 2 uM to 0.1nM, or extecan ranging from 20 uM to 0.03 nM were added to the cells. Plates were then incubated at 37°C for 96h. Cell Titer Glo (CTG) (40 ul per well) was subsequently added to the plates. Luciferase reading was collected 5min after and analyzed by Microplatereaders. All readings were normalized as percentage of viable cells in the untreated control wells and theICso yalues were calculated by Prism software.
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| In Vitro Model | Renal cell carcinoma | 786-O cells | CVCL_1051 | ||