Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0TJWGK
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| ADC Name |
YTH24.5-SG3249
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| Synonyms |
YTH24.5-SG3249
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| Organization |
CL Great Ormond Street Institute of Child Health, Zayed Centre of Research, 20 Guilford Street, London WC1N 1DZ, UK; UCL Cancer Institute, 72 Huntley Street, London, UK.
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| Drug Status |
Investigative
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| Drug-to-Antibody Ratio |
2
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| Structure |
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| Antibody Name |
YTH24.5
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Antibody Info | Antigen Name |
Undisclosed
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| Payload Name |
Undisclosed
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| Therapeutic Target |
Stimulator of interferon genes protein (STING1)
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Target Info | ||||
| Linker Name |
Undisclosed
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| Conjugate Type |
Random conjugation through reduced inter-chain cysteines.
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| Combination Type |
SG3376
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General Information of The ADMET Data Related to This ADC(2027 Update)
Excretion
| Standard Type | Value | Units | Description | Reference |
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| Elimination Half-Life (t1/2) | 1.5 | day |
Conditioning agents for SCT or gene therapy require a short half-life (t½) to avoid depleting the incoming HSCs. We performed pharmacokinetic (PK) studies in non-humanized NSG mice to determine the t½ of ADCs and their stability in vivo. Non-compartmental analysis on serial serum samples revealed that YTH24.5-SG3249 had a t½ of ~1.5 days in non-humanized NSG mice
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[1] |
General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
Full List of Activity Data of This Antibody-drug Conjugate
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | 0.03 pM | Positive CD45 expression (CD45+++/++) | ||
| Method Description |
Cells at 0.5 × 105/mL were cultured for 5 days in mAb or ADC or medium (in triplicate wells) in wells of flat-bottom 96-well plates. PrestoBlue Cell Viability reagent (Thermo Fisher Scientific) was added and incubated for 1.5 h. Fluorescence intensity from each well was detected using a FLUOstar OPTIMA microplate reader (BMG Labtech, Aylesbury, UK) using excitation filter of 560-10 and emission filter of 590-10, and gain at 1,500. Data were plotted using GraphPad Prism software, and sigmoid dose-response non-linear regression was carried out to determine IC50 values.
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| In Vitro Model | Acute erythroid leukemia | OCIM1 cells | CVCL_2149 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | 0.213 pM | Positive CD45 expression (CD45+++/++) | ||
| Method Description |
Cells at 0.5 × 105/mL were cultured for 5 days in mAb or ADC or medium (in triplicate wells) in wells of flat-bottom 96-well plates. PrestoBlue Cell Viability reagent (Thermo Fisher Scientific) was added and incubated for 1.5 h. Fluorescence intensity from each well was detected using a FLUOstar OPTIMA microplate reader (BMG Labtech, Aylesbury, UK) using excitation filter of 560-10 and emission filter of 590-10, and gain at 1,500. Data were plotted using GraphPad Prism software, and sigmoid dose-response non-linear regression was carried out to determine IC50 values.
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| In Vitro Model | T acute lymphoblastic leukemia | Jurkat cells | CVCL_0065 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | > 6000 pM | Negative CD45 expression (CD45-) | ||
| Method Description |
Cells at 0.5 × 105/mL were cultured for 5 days in mAb or ADC or medium (in triplicate wells) in wells of flat-bottom 96-well plates. PrestoBlue Cell Viability reagent (Thermo Fisher Scientific) was added and incubated for 1.5 h. Fluorescence intensity from each well was detected using a FLUOstar OPTIMA microplate reader (BMG Labtech, Aylesbury, UK) using excitation filter of 560-10 and emission filter of 590-10, and gain at 1,500. Data were plotted using GraphPad Prism software, and sigmoid dose-response non-linear regression was carried out to determine IC50 values.
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| In Vitro Model | Normal | 293T cells | CVCL_0063 | ||
References