General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0OJPML
ADC Name
CN116916962A-ADC-B16
Synonyms
ADC-B16
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Organization
TAKEDA PHARMACEUTICAL COMPANY LIMITED
Drug Status
Investigative
Drug-to-Antibody Ratio
4.1
Structure
Antibody Name
hIgG1
 Antibody Info 
Antigen Name
Undisclosed
Payload Name
Compound I-5c
 Payload Info 
Linker Name
CN116916962A-C-41-linker
 Linker Info 
Conjugate Type
Random conjugation through reduced inter-chain cysteines.
Combination Type
C-41
General Information of The ADMET Data Related to This ADC(2027 Update)
Absorption
Click To Hide/Show 1 Absorption Data Related to This Level
Standard Type Value Units Description Reference
Area Under the Concentration-Time Curve (AUC) 12300 h&#42nM
For in vivo evaluation of the ADCs in naive Balb/C mouse, female Balb/C mice at 6-8weeks of age were used.Pharmacokinetics of the ADCs (0.05mg/kg) were studied following injection of ADCs into Balb/C mice.

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[1]
Distribution
Click To Hide/Show 1 Distribution Data Related to This Level
Standard Type Value Units Description Reference
Area Under the Concentration-Time Curve (AUC) 12300 h&#42nM
For in vivo evaluation of the ADCs in naive Balb/C mouse, female Balb/C mice at 6-8weeks of age were used.Pharmacokinetics of the ADCs (0.05mg/kg) were studied following injection of ADCs into Balb/C mice.

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[1]
Metabolism
Click To Hide/Show 1 Metabolism Data Related to This Level
Standard Type Value Units Description Reference
Area Under the Concentration-Time Curve (AUC) 12300 h&#42nM
For in vivo evaluation of the ADCs in naive Balb/C mouse, female Balb/C mice at 6-8weeks of age were used.Pharmacokinetics of the ADCs (0.05mg/kg) were studied following injection of ADCs into Balb/C mice.

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[1]
Excretion
Click To Hide/Show 2 Excretion Data Related to This Level
Standard Type Value Units Description Reference
Elimination Half-Life (t1/2) 58 h
For in vivo evaluation of the ADCs in naive Balb/C mouse, female Balb/C mice at 6-8weeks of age were used.Pharmacokinetics of the ADCs (0.05mg/kg) were studied following injection of ADCs into Balb/C mice.

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[1]
Area Under the Concentration-Time Curve (AUC) 12300 h&#42nM
For in vivo evaluation of the ADCs in naive Balb/C mouse, female Balb/C mice at 6-8weeks of age were used.Pharmacokinetics of the ADCs (0.05mg/kg) were studied following injection of ADCs into Balb/C mice.

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[1]
General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Effective Concentration (EC50) 
2.46
nM
CVCL_0006
Acute monoblastic/monocytic leukemia, Childhood acute monocytic leukemia
Full List of Activity Data of This Antibody-drug Conjugate
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) 2.46 nM High hCCR2 expression (hCCR2+++)
Method Description
THP 1, 15,000cells/254uL per welld were plated at set in 384 well flat plate, in the appropriate growth media. The cell plates were dosed with 5uL of the hCCR2 targeting-ADC samples and then incubated at 37°C for 20 hours. At the end of the incubation 10uL/well of the QUANTJ-LucTM (InvivoGenftrep-qlc1) were added and luminescence was measured immediately using the LeadSeeker.

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In Vitro Model Acute monoblastic/monocytic leukemia, Childhood acute monocytic leukemia THP1 cells CVCL_0006
References
Ref 1 Antibody-drug conjugates