Linker Information
General Information of This Linker
| Linker ID |
LIN0RYKTT
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| Linker Name |
A polyethylene glycol-modified branched-link agent
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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 |
C49H80N6O16
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| Isosmiles |
C[C@H](NC([C@@H](NC([C@@H](NC(CCCCCN1C(C=CC1=O)=O)=O)CCCCNC(CCOCCOCCOCCOCCOCCOCCOCCOC)=O)=O)C(C)C)=O)C(NC2=CC=C(CO)C=C2)=O
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| InChI |
InChI=1S/C49H80N6O16/c1-37(2)46(49(63)51-38(3)47(61)52-40-14-12-39(36-56)13-15-40)54-48(62)41(53-43(58)11-6-5-9-20-55-44(59)16-17-45(55)60)10-7-8-19-50-42(57)18-21-65-24-25-67-28-29-69-32-33-71-35-34-70-31-30-68-27-26-66-23-22-64-4/h12-17,37-38,41,46,56H,5-11,18-36H2,1-4H3,(H,50,57)(H,51,63)(H,52,61)(H,53,58)(H,54,62)/t38-,41-,46-/m0/s1
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| InChIKey |
AHVBLALLZOGMCT-GSYYMGFTSA-N
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| Pharmaceutical Properties |
Molecule Weight
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1009.205
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Polar area
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276.95
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Complexity
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1618.296769
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xlogp Value
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1.1723
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Heavy Count
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71
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Rot Bonds
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44
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Hbond acc
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16
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Hbond Donor
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6
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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
40285886 7300-LP2004 [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) |
39.74 nM
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| Method Description |
SHP-77 cells were grown in RPMI-1640 medium supplemented with 10% FBS and 1 ug/mL puromycin at 37 °C in a 5% CO2 incubator. SHP-77 cells were dissociated using TrypLETM Express Enzyme (Thermo Fisher Scientific, Waltham, MA, USA) and, after counting, the cells were resuspended in RPMI-1640 medium supplemented with 10% FBS at a density of 3 × 104 cells/mL. The cells were plated in 96-well plates and incubated at 37 °C for 24 h. ADCs and payloads were diluted separately and added to the 96-well cell culture plates containing cells, followed by incubation in a 5% CO2 incubator for 5 days. A multifunctional microplate reader was used, and the absorbance was measured at 450 nm with a reference wavelength of 630 nm. The IC50 values were calculated using GraphPad Prism 10.1.2 software.
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| In Vitro Model | Small cell lung carcinoma | SHP-77 cells | CVCL_1693 | ||
References
