Payload Information

General Information of This Payload
Payload ID
PAY0WKBCR
Name
PNU-159682
Synonyms
PNU-159682; 202350-68-3; UNII-CQ5A9ZNT7C; CQ5A9ZNT7C; PNU159682; PNU 159682; (8S,10S)-6,8,11-Trihydroxy-8-(2-hydroxyacetyl)-1-methoxy-10-(((1S,3R,4aS,9S,9aR,10aS)-9-methoxy-1-methyloctahydro-1H-pyrano[4',3':4,5]oxazolo[2,3-c][1,4]oxazin-3-yl)oxy)-7,8,9,10-tetrahydrotetracene-5,12-dione; (7S,9S)-6,9,11-Trihydroxy-9-(2-hydroxyacetyl)-4-methoxy-7-[[(2S,4R,6S,7S,9R,10S)-10-methoxy-6-methyl-5,8,11-trioxa-1-azatricyclo[7.4.0.02,7]tridecan-4-yl]oxy]-8,10-dihydro-7H-tetracene-5,12-dione; (8S,10S)-7,8,9,10-Tetrahydro-6,8,11-trihydroxy-8-(2-hydroxyacetyl)-1-methoxy-10-(((1S,3R,4aS,9S,9aR,10aS)-octahydro-9-methoxy-1-methyl-1H-pyrano(4',3':4,5)oxazolo(2,3-C)(1,4)oxazin-3-yl)oxy)-5,12-naphthacenedione; 5,12-Naphthacenedione, 7,8,9,10-tetrahydro-6,8,11-trihydroxy-8-(2-hydroxyacetyl)-1-methoxy-10-(((1S,3R,4aS,9S,9aR,10aS)-octahydro-9-methoxy-1-methyl-1H-pyrano(4',3':4,5)oxazolo(2,3-C)(1,4)oxazin-3-yl)oxy)-, (8S,10S)-; (8S,10S)-7,8,9,10-Tetrahydro-6,8,11-trihydroxy-8-(2-hydroxyacetyl)-1-methoxy-10-[[(1S,3R,4aS,9S,9aR,10aS)-octahydro-9-methoxy-1-methyl-1H-pyrano[4',3':4,5]oxazolo[2,3-c][1,4]oxazin-3-yl]oxy]-5,12-naphthacenedione; SCHEMBL3801318; CHEMBL4777727; SLURUCSFDHKXFR-WWMWMSKMSA-N; EX-A3364; CS-3298; BP-29359; HY-16700; MS-30920; A903771; (8S,10S)-6,8,11-trihydroxy-8-(2-hydroxyacetyl)-1-methoxy-10-{[(2S,4R,6S,7S,9R,10S)-10-methoxy-6-methyl-5,8,11-trioxa-1-azatricyclo[7.4.0.0,tridecan-4-yl]oxy}-5,7,8,9,10,12-hexahydrotetracene-5,12-dione; (8S,10S)-6,8,11-trihydroxy-8-(hydroxyacetyl)-1-methoxy-10-{[(1S,3R,4aS,9S,9aR,10aS)-9-methoxy-1-methyloctahydro-1H-pyrano[4',3':4,5] [1,3] oxazolo[2,3-c][1,4]oxazin-3-yl]oxy}-7,8,9,10-tetrahydrotetracene-5,12-dione; (8S,10S)-6,8,11-trihydroxy-8-(hydroxyacetyl)-1-methoxy-10-{[(1S,3R,4aS,9S,9aR,10aS)-9-methoxy-1-methyloctahydro-1H-pyrano[4',3':4,5][1,3]oxazolo[2,3-c][1,4]oxazin-3-yl]oxy}-7,8,9,10-tetrahydrotetracene-5,12-dione
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Target DNA topoisomerase 2-alpha (TOP2A)
 Target Info 
Structure
Formula
C32H35NO13
Isosmiles
C[C@H]1[C@@H]2[C@H](C[C@@H](O1)O[C@H]3C[C@@](CC4=C3C(=C5C(=C4O)C(=O)C6=C(C5=O)C(=CC=C6)OC)O)(C(=O)CO)O)N7CCO[C@@H]([C@H]7O2)OC
PubChem CID
9874188
InChI
InChI=1S/C32H35NO13/c1-13-29-16(33-7-8-43-31(42-3)30(33)46-29)9-20(44-13)45-18-11-32(40,19(35)12-34)10-15-22(18)28(39)24-23(26(15)37)25(36)14-5-4-6-17(41-2)21(14)27(24)38/h4-6,13,16,18,20,29-31,34,37,39-40H,7-12H2,1-3H3/t13-,16-,18-,20-,29+,30+,31-,32-/m0/s1
InChIKey
SLURUCSFDHKXFR-WWMWMSKMSA-N
IUPAC Name
(7S,9S)-6,9,11-trihydroxy-9-(2-hydroxyacetyl)-4-methoxy-7-[[(2S,4R,6S,7S,9R,10S)-10-methoxy-6-methyl-5,8,11-trioxa-1-azatricyclo[7.4.0.02,7]tridecan-4-yl]oxy]-8,10-dihydro-7H-tetracene-5,12-dione
Pharmaceutical Properties
Molecule Weight
641.6
Polar area
191
Complexity
1200
xlogp Value
2.4
Heavy Count
46
Rot Bonds
6
Hbond acc
14
Hbond Donor
4
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
SO-N102 [Phase 1/2 (discontinued)]
 ADC Info 
Identified from the Human Clinical Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Patients Enrolled
Exclusions encompass recent radiotherapy (<14 days), severe comorbidities (e.g., gastric ulcers, pulmonary fibrosis), uncontrolled CNS metastases, grade ≥2 neuropathy, active infections, cardiac risks (e.g., arrhythmias, bradycardia), major surgery (<28 days), recent transfusions, or live vaccinations (<30 days). Parts B/D exclude patients contraindicated for first-line SoC. Additional investigator-assessed contraindications may apply.

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Administration Dosage
Starting dose of SOT102 is 0.032 mg/kg. Dose levels are to be escalated according modified Fibonacci scheme.
Related Clinical Trial
NCT Number NCT05525286  Phase Status PHASE1|||PHASE2
Clinical Description
A Multicentric Phase 1/2 Trial to Evaluate the Safety and Efficacy of SOT102 as Monotherapy and in Combination With Standard of Care Treatment in Patients With Gastric and Pancreatic Adenocarcinoma
Primary Endpoint
Parts A and B focus on determining the maximum tolerated dose (MTD) and recommended phase 2 dose (RP2D) of SOT102, defined as the highest dose below the level causing ≥33% dose-limiting toxicities (DLTs). Parts C and D evaluate efficacy via objective response rate (ORR) per RECIST 1.1, alongside safety assessments including DLTs, treatment-emergent adverse events (TEAEs), serious AEs (SAEs), and lab abnormalities. Key outcomes also include pharmacokinetics (PK), immunogenicity (anti-drug antibodies), duration of response (DoR), progression-free survival (PFS), clinical benefit rate (CBR), and overall survival (OS).

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Other Endpoint
Inclusion criteria require adequate hematologic (ANC ≥1.5×109/L), hepatic (bilirubin ≤1.5×ULN), renal (CrCl ≥60 mL/min), and coagulation (INR ≤1.5×ULN) function, ECOG ≤1, and life expectancy ≥3 months. Parts A-D specify disease-specific eligibility: Parts A/B include advanced/metastatic pancreatic adenocarcinoma; Part C mandates prior systemic therapy; Part D aligns with Part B but excludes contraindications to first-line SoC. Female patients must adhere to contraception protocols.

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Experiment 2 Reporting the Activity Date of This ADC [3]
Related Clinical Trial
NCT Number NCT05525286  Phase Status Phase 1
Clinical Description
A multicentric phase 1/2 trial to evaluate the safety and efficacy of SOT102 as monotherapy and in combination with standard of care treatment in patients with gastric and pancreatic adenocarcinoma.
NBE-002 [Phase 1/2 (discontinued)]
 ADC Info 
Identified from the Human Clinical Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Patients Enrolled
Eligibility requires age ≥18, progressive advanced tumors (Phase 1: any solid tumor refractory to standard therapy; Phase 2: TNBC ≤3L or other solid tumors ≤3L), measurable disease (Phase 2 only), ECOG 0-2 (Phase 1) or 0-1 (Phase 2), and adequate organ function. Key exclusions include prior ROR1-targeting therapy, active CNS metastases, unresolved Grade >1 toxicity from prior treatments, recent anticancer therapies/surgeries, significant comorbidities, and secondary malignancies within 3 years.

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Administration Dosage
NBE-002 will be given intravenously on Day 1 of repeated 28-day cycles.
Related Clinical Trial
NCT Number NCT04441099  Phase Status PHASE1|||PHASE2
Clinical Description
A First-in-Human, Phase 1/2 Study of NBE-002, an Anti-ROR1 Antibody Drug Conjugate, in Patients With Advanced Solid Tumors
Primary Endpoint
The Phase 1 portion focuses on determining the RP2D through DLT assessments over 48 months, while Phase 2 evaluates anti-tumor activity per RECIST v1.1 for up to 60 months.
Other Endpoint
Safety monitoring (CTCAE v5.0) and preliminary efficacy (RECIST v1.1) run through 48-60 months, with additional PK (NBE-002 concentrations) and immunogenicity (anti-drug antibodies) profiling.
HuIgG1-19 [Investigative]
 ADC Info 
Discovered Using Patient-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 13.33% Positive CD46 expression (CD46 +++/++)
Method Description
In vivo efficacy of PNU-conjugated ADCs in NSCLC LU253 PDX subcutaneous models in NOD/SCID mice. A single dose of 1.0 mg/kg HuIgG1-19 ADC.
In Vivo Model Non-small cell lung cancer PDX model (PDX: LU253 PDX)
Experiment 2 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 21.34% Positive CD46 expression (CD46 +++/++)
Method Description
In vivo efficacy of PNU-conjugated ADCs in colorectal CR188 PDX subcutaneous models in NOD/SCID mice. A single dose of 1.0 mg/kg HuIgG1-19 ADC.
In Vivo Model Colorectal cancer PDX model (PDX: CR188 PDX)
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Effective Concentration (EC50) > 3 nM Positive CD46 expression (CD46 +++/++)
Method Description
Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model Uterine sarcoma MES-SA cells CVCL_1404
Experiment 2 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Effective Concentration (EC50)
3.8 nM
Positive CD46 expression (CD46 +++/++)
Method Description
Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model Normal HEK293T cells CVCL_0063
HCD46-19 [Investigative]
 ADC Info 
Discovered Using Patient-derived Xenograft Model
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 52.34% Positive CD46 expression (CD46 +++/++)
Method Description
In vivo efficacy of PNU-conjugated ADCs in NSCLC LU253 PDX subcutaneous models in NOD/SCID mice. A single dose of 0.5 mg/kg hCD46-19 ADC.
In Vivo Model Non-small cell lung cancer PDX model (PDX: LU253 PDX)
Experiment 2 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 77.34% Positive CD46 expression (CD46 +++/++)
Method Description
In vivo efficacy of PNU-conjugated ADCs in colorectal CR188 PDX subcutaneous models in NOD/SCID mice. A single dose of 0.5 mg/kg hCD46-19 ADC.
In Vivo Model Colorectal cancer PDX model (PDX: CR188 PDX)
Experiment 3 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 86.67% Positive CD46 expression (CD46 +++/++)
Method Description
In vivo efficacy of PNU-conjugated ADCs in colorectal CR188 PDX subcutaneous models in NOD/SCID mice. A single dose of 1.0 mg/kg hCD46-19 ADC.
In Vivo Model Colorectal cancer PDX model (PDX: CR188 PDX)
Experiment 4 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 90.48% Positive CD46 expression (CD46 +++/++)
Method Description
In vivo efficacy of PNU-conjugated ADCs in NSCLC LU253 PDX subcutaneous models in NOD/SCID mice. A single dose of 1.0 mg/kg hCD46-19 ADC.
In Vivo Model Non-small cell lung cancer PDX model (PDX: LU253 PDX)
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Effective Concentration (EC50)
47 pM
Positive CD46 expression (CD46 +++/++)
Method Description
Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model Normal HEK293T cells CVCL_0063
Experiment 2 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Effective Concentration (EC50) > 3 nM Positive CD46 expression (CD46 +++/++)
Method Description
Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model Uterine sarcoma MES-SA cells CVCL_1404
Trastuzumab-PNUEDAGly5 [Investigative]
 ADC Info 
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100% Positive HER2 expression (HER2 +++/++)
Method Description
1,000,000 EMT6 mouse breast cancer cells expressing human HER-2 previously determined to be suitable for in vivo growth, were implanted into theright mammary fat pads of female Balb/c mice. Animals were treated onthe same day (day 13) and 7 days later (day 20) byintravenous injection of the reference ADC Kadcyla (15 mg/kg), Trastuzumab-PNU-EDA-Glys (1 mg/kg) or vehicle control.

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In Vivo Model EMT6 CDX model (Expressing hHER2)
In Vitro Model Mammary gland malignant neoplasms EMT6 cells (High HER2 expression) CVCL_1923
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [8]
Efficacy Data Half Maximal Effective Concentration (EC50)
6.9 ng/mL
High CD30 expression (CD30 +++)
Method Description
Dose response of the cytotoxic effects of the indicated ADCs on human Non-Hodgkin lymphoma cell line Karpas-299, and on human Hodgkin lymphoma cell line L428 cells.
In Vitro Model ALK-positive anaplastic large cell lymphoma Karpas-299 cells CVCL_1324
Experiment 2 Reporting the Activity Date of This ADC [8]
Efficacy Data Half Maximal Effective Concentration (EC50) < 10 ug/mL Low CD30 expression (CD30 +)
Method Description
Dose response of the cytotoxic effects of the indicated ADCs on human Non-Hodgkin lymphoma cell line Karpas-299, and on human Hodgkin lymphoma cell line L428 cells.
In Vitro Model Hodgkin lymphoma L-428 cells CVCL_1361
CAC10-Gly5-PNU [Investigative]
 ADC Info 
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [6]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100% High CD30 expression (CD30+++)
Method Description
CD30 Karpas-299 cells were either transplanted subcutaneously into NSG, or into CB17.SCID mice. Mice were treated intravenously 3 times weekly with 1 mg/kg preparations, beginning one day post randomization, when the tumors had reached a size ranging between 100 and 150 mm3.
In Vivo Model Non-Hodgkin's lymphoma CDX model
In Vitro Model ALK-positive anaplastic large cell lymphoma Karpas-299 cells CVCL_1324
Experiment 2 Reporting the Activity Date of This ADC [6]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100% High CD30 expression (CD30+++)
Method Description
CD30 Karpas-299 cells were either transplanted subcutaneously into NSG, or into CB17.SCID mice. Mice were treated intravenously 3 times weekly with 1 mg/kg preparations, beginning one day post randomization, when the tumors had reached a size ranging between 100 and 150 mm3.
In Vivo Model Non-Hodgkin's lymphoma CDX model
In Vitro Model ALK-positive anaplastic large cell lymphoma Karpas-299 cells CVCL_1324
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [6]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.8 ng/mL
High CD30 expression (CD30+++)
Method Description
Briefly, cells were plated on 96-well plates in 75 uL growth medium and grown at 37°C in a humidified incubator in a 7.5% CO2 atmosphere. After one day incubation, 25 uL of 3.5-fold serial dilutions of each ADC in growth medium were added, typically resulting in final ADC concentrations from 20 ug/mL to 0.02 ng/mL.
In Vitro Model ALK-positive anaplastic large cell lymphoma Karpas-299 cells CVCL_1324
Experiment 2 Reporting the Activity Date of This ADC [6]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
4.8 ng/mL
Negative CD30 expression (CD30-)
Method Description
Briefly, cells were plated on 96-well plates in 75 uL growth medium and grown at 37°C in a humidified incubator in a 7.5% CO2 atmosphere. After one day incubation, 25 uL of 3.5-fold serial dilutions of each ADC in growth medium were added, typically resulting in final ADC concentrations from 20 ug/mL to 0.02 ng/mL.
In Vitro Model B acute lymphoblastic leukemia Reh cells CVCL_1650
Tras-Gly5-EDA-Pnu [Investigative]
 ADC Info 
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [6]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100% High HER2 expression (HER2+++; 170,000 HER2 molecules/cell)
Method Description
JIMT-1 cells were transplanted subcutaneously into CB17.SCID mice and tumors were allowed to grow to a volume of 100-150 mm3. Mice were then treated intravenously 3 times weekly with the 1 mg/kg ADC preparations.
In Vivo Model Trastuzumab-resistant breast cancer CDX model
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [6]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
2.7 ng/mL
High HER2 expression (HER2+++; 694,000 HER2 molecules/cell)
Method Description
Briefly, cells were plated on 96-well plates in 75 uL growth medium and grown at 37°C in a humidified incubator in a 7.5% CO2 atmosphere. After one day incubation, 25 uL of 3.5-fold serial dilutions of each ADC in growth medium were added, typically resulting in final ADC concentrations from 20 ug/mL to 0.02 ng/mL.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [6]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
14.7 ng/mL
Moderate HER2 expression (HER2++; 32,000 HER2 molecules/cell)
Method Description
Briefly, cells were plated on 96-well plates in 75 uL growth medium and grown at 37°C in a humidified incubator in a 7.5% CO2 atmosphere. After one day incubation, 25 uL of 3.5-fold serial dilutions of each ADC in growth medium were added, typically resulting in final ADC concentrations from 20 ug/mL to 0.02 ng/mL.
In Vitro Model Invasive breast carcinoma T-47D cells CVCL_0553
Tras-Gly3-Vakl-Cit-PAB-PNU-159682 [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [6]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.24 ng/mL
High HER2 expression (HER2+++; 694,000 HER2 molecules/cell)
Method Description
Briefly, cells were plated on 96-well plates in 75 uL growth medium and grown at 37°C in a humidified incubator in a 7.5% CO2 atmosphere. After one day incubation, 25 uL of 3.5-fold serial dilutions of each ADC in growth medium were added, typically resulting in final ADC concentrations from 20 ug/mL to 0.02 ng/mL.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [6]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
12 ng/mL
Moderate HER2 expression (HER2++; 32,000 HER2 molecules/cell)
Method Description
Briefly, cells were plated on 96-well plates in 75 uL growth medium and grown at 37°C in a humidified incubator in a 7.5% CO2 atmosphere. After one day incubation, 25 uL of 3.5-fold serial dilutions of each ADC in growth medium were added, typically resulting in final ADC concentrations from 20 ug/mL to 0.02 ng/mL.
In Vitro Model Invasive breast carcinoma T-47D cells CVCL_0553
HuXBR1-402-G5-PNU [Clinical candidate]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [7]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.27 ng/mL
Positive ROR1 expression (ROR1+++/++)
Method Description
Cell lines obtained from ATCC were serum starved for 16 hours and reintroduced to full serum media supplemented huXBR1-402-G5-PNU for 72 hours. Viability was measured by using MTS assays, and relative light unit (RLU) values for each dose were generated after 72 hours of treatment in 2 independent experiments.
In Vitro Model Childhood B acute lymphoblastic leukemia Kasumi-2 cells CVCL_0590
Experiment 2 Reporting the Activity Date of This ADC [7]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
75.68 ng/mL
Positive ROR1 expression (ROR1+++/++)
Method Description
Cell lines obtained from ATCC were serum starved for 16 hours and reintroduced to full serum media supplemented huXBR1-402-G5-PNU for 72 hours. Viability was measured by using MTS assays, and relative light unit (RLU) values for each dose were generated after 72 hours of treatment in 2 independent experiments.
In Vitro Model Childhood B acute lymphoblastic leukemia 697 cells CVCL_0079
HCD46-29 [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Effective Concentration (EC50)
41 pM
Positive CD46 expression (CD46 +++/++)
Method Description
Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model Uterine sarcoma MES-SA cells CVCL_1404
Experiment 2 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Effective Concentration (EC50)
1.6 nM
Positive CD46 expression (CD46 +++/++)
Method Description
Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model Normal HEK293T cells CVCL_0063
HCD46-25 [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Effective Concentration (EC50)
95 pM
Positive CD46 expression (CD46 +++/++)
Method Description
Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model Uterine sarcoma MES-SA cells CVCL_1404
Experiment 2 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Effective Concentration (EC50)
5.19 nM
Positive CD46 expression (CD46 +++/++)
Method Description
Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model Normal HEK293T cells CVCL_0063
HuIgG1-25 [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Effective Concentration (EC50) > 1000 pM Positive CD46 expression (CD46 +++/++)
Method Description
Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model Normal HEK293T cells CVCL_0063
Experiment 2 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Effective Concentration (EC50) > 3 nM Positive CD46 expression (CD46 +++/++)
Method Description
Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model Uterine sarcoma MES-SA cells CVCL_1404
HuIgG1-26 [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Effective Concentration (EC50)
1000 pM
Positive CD46 expression (CD46 +++/++)
Method Description
Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model Uterine sarcoma MES-SA cells CVCL_1404
Experiment 2 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Effective Concentration (EC50)
1.1 nM
Positive CD46 expression (CD46 +++/++)
Method Description
Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model Normal HEK293T cells CVCL_0063
HCD46-26 [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.1 nM
Positive CD46 expression (CD46 +++/++)
Method Description
Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model Uterine sarcoma MES-SA cells CVCL_1404
Experiment 2 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.19 nM
Positive CD46 expression (CD46 +++/++)
Method Description
Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model Normal HEK293T cells CVCL_0063
HuIgG1-29 [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Effective Concentration (EC50)
1.4 nM
Positive CD46 expression (CD46 +++/++)
Method Description
Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model Uterine sarcoma MES-SA cells CVCL_1404
Experiment 2 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Effective Concentration (EC50)
2 nM
Positive CD46 expression (CD46 +++/++)
Method Description
Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model Normal HEK293T cells CVCL_0063
Brentuximab-PNUEDAGly5 [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Effective Concentration (EC50)
4.8 ng/mL
High HER2 expression (HER2 +++)
Method Description
For this, cells were plated on 96 well plates in 100 ul DMEM/10% FCS at adensity of 104 cells per well and assays were performed.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Effective Concentration (EC50)
11 ng/mL
Low HER2 expression (HER2 +)
Method Description
For this, cells were plated on 96 well plates in 100 ul DMEM/10% FCS at adensity of 104 cells per well and assays were performed.
In Vitro Model Invasive breast carcinoma T-47D cells CVCL_0553
ZA202500202A D04-F404-LP27 [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [9]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.017 nM
Positive ROR1 expression (ROR1+++/++)
Method Description
Ntera-2 cell at 625 cells/25 pL were seeded in a 384-well plat. ADCs were formulated at 2x starting concentration. Filter sterilized samples were serial diluted (1:3) under sterile conditions and added onto cells in triplicates. For cell viability measurement, 30 microliter of Cell Titer-Glo@ reagent (Promega Corp, Madison, WI) was added into each well, and plates processed as per product instructions.

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In Vitro Model Embryonal carcinoma Ntera-2 cells CVCL_0034
Experiment 2 Reporting the Activity Date of This ADC [9]
Efficacy Data Half Maximal Effective Concentration (EC50) > 10 nM Negative ROR1 expression (ROR1-)
Method Description
MCF-7 cells at 625 cells/25 pL were seeded in a 384-well plat. ADCs were formulated at 2x starting concentration. Filter sterilized samples were serial diluted (1:3) under sterile conditions and added onto cells in triplicates. For cell viability measurement, 30 microliter of Cell Titer-Glo@ reagent (Promega Corp, Madison, WI) was added into each well, and plates processed as per product instructions.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
ZA202500202A D04-F404-LP30 [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [9]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.043 nM
Positive ROR1 expression (ROR1+++/++)
Method Description
Ntera-2 cell at 625 cells/25 pL were seeded in a 384-well plat. ADCs were formulated at 2x starting concentration. Filter sterilized samples were serial diluted (1:3) under sterile conditions and added onto cells in triplicates. For cell viability measurement, 30 microliter of Cell Titer-Glo@ reagent (Promega Corp, Madison, WI) was added into each well, and plates processed as per product instructions.

   Click to Show/Hide
In Vitro Model Embryonal carcinoma Ntera-2 cells CVCL_0034
Experiment 2 Reporting the Activity Date of This ADC [9]
Efficacy Data Half Maximal Effective Concentration (EC50) > 10 nM Negative ROR1 expression (ROR1-)
Method Description
MCF-7 cells at 625 cells/25 pL were seeded in a 384-well plat. ADCs were formulated at 2x starting concentration. Filter sterilized samples were serial diluted (1:3) under sterile conditions and added onto cells in triplicates. For cell viability measurement, 30 microliter of Cell Titer-Glo@ reagent (Promega Corp, Madison, WI) was added into each well, and plates processed as per product instructions.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
ZA202500202A D04-F404-LP25 [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [9]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.075 nM
Positive ROR1 expression (ROR1+++/++)
Method Description
Ntera-2 cell at 625 cells/25 pL were seeded in a 384-well plat. ADCs were formulated at 2x starting concentration. Filter sterilized samples were serial diluted (1:3) under sterile conditions and added onto cells in triplicates. For cell viability measurement, 30 microliter of Cell Titer-Glo@ reagent (Promega Corp, Madison, WI) was added into each well, and plates processed as per product instructions.

   Click to Show/Hide
In Vitro Model Embryonal carcinoma Ntera-2 cells CVCL_0034
Experiment 2 Reporting the Activity Date of This ADC [9]
Efficacy Data Half Maximal Effective Concentration (EC50) > 10 nM Negative ROR1 expression (ROR1-)
Method Description
MCF-7 cells at 625 cells/25 pL were seeded in a 384-well plat. ADCs were formulated at 2x starting concentration. Filter sterilized samples were serial diluted (1:3) under sterile conditions and added onto cells in triplicates. For cell viability measurement, 30 microliter of Cell Titer-Glo@ reagent (Promega Corp, Madison, WI) was added into each well, and plates processed as per product instructions.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
ZA202500202A D04-F404-LP32 [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [9]
Efficacy Data Half Maximal Effective Concentration (EC50)
2.955 nM
Positive ROR1 expression (ROR1+++/++)
Method Description
Ntera-2 cell at 625 cells/25 pL were seeded in a 384-well plat. ADCs were formulated at 2x starting concentration. Filter sterilized samples were serial diluted (1:3) under sterile conditions and added onto cells in triplicates. For cell viability measurement, 30 microliter of Cell Titer-Glo@ reagent (Promega Corp, Madison, WI) was added into each well, and plates processed as per product instructions.

   Click to Show/Hide
In Vitro Model Embryonal carcinoma Ntera-2 cells CVCL_0034
Experiment 2 Reporting the Activity Date of This ADC [9]
Efficacy Data Half Maximal Effective Concentration (EC50) > 10 nM Negative ROR1 expression (ROR1-)
Method Description
MCF-7 cells at 625 cells/25 pL were seeded in a 384-well plat. ADCs were formulated at 2x starting concentration. Filter sterilized samples were serial diluted (1:3) under sterile conditions and added onto cells in triplicates. For cell viability measurement, 30 microliter of Cell Titer-Glo@ reagent (Promega Corp, Madison, WI) was added into each well, and plates processed as per product instructions.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
ZA202500202A D04-Y180/F404-LP32 [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [9]
Efficacy Data Half Maximal Effective Concentration (EC50) > 10 nM Positive ROR1 expression (ROR1+++/++)
Method Description
Ntera-2 cell at 625 cells/25 pL were seeded in a 384-well plat. ADCs were formulated at 2x starting concentration. Filter sterilized samples were serial diluted (1:3) under sterile conditions and added onto cells in triplicates. For cell viability measurement, 30 microliter of Cell Titer-Glo@ reagent (Promega Corp, Madison, WI) was added into each well, and plates processed as per product instructions.

   Click to Show/Hide
In Vitro Model Embryonal carcinoma Ntera-2 cells CVCL_0034
Experiment 2 Reporting the Activity Date of This ADC [9]
Efficacy Data Half Maximal Effective Concentration (EC50) > 10 nM Negative ROR1 expression (ROR1-)
Method Description
MCF-7 cells at 625 cells/25 pL were seeded in a 384-well plat. ADCs were formulated at 2x starting concentration. Filter sterilized samples were serial diluted (1:3) under sterile conditions and added onto cells in triplicates. For cell viability measurement, 30 microliter of Cell Titer-Glo@ reagent (Promega Corp, Madison, WI) was added into each well, and plates processed as per product instructions.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
ZA202500202A D04-F404-LP31 [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [9]
Efficacy Data Half Maximal Effective Concentration (EC50) > 10 nM Positive ROR1 expression (ROR1+++/++)
Method Description
Ntera-2 cell at 625 cells/25 pL were seeded in a 384-well plat. ADCs were formulated at 2x starting concentration. Filter sterilized samples were serial diluted (1:3) under sterile conditions and added onto cells in triplicates. For cell viability measurement, 30 microliter of Cell Titer-Glo@ reagent (Promega Corp, Madison, WI) was added into each well, and plates processed as per product instructions.

   Click to Show/Hide
In Vitro Model Embryonal carcinoma Ntera-2 cells CVCL_0034
Experiment 2 Reporting the Activity Date of This ADC [9]
Efficacy Data Half Maximal Effective Concentration (EC50) > 10 nM Negative ROR1 expression (ROR1-)
Method Description
MCF-7 cells at 625 cells/25 pL were seeded in a 384-well plat. ADCs were formulated at 2x starting concentration. Filter sterilized samples were serial diluted (1:3) under sterile conditions and added onto cells in triplicates. For cell viability measurement, 30 microliter of Cell Titer-Glo@ reagent (Promega Corp, Madison, WI) was added into each well, and plates processed as per product instructions.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
ZA202500202A D04-F404-LP24 [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [9]
Efficacy Data Half Maximal Effective Concentration (EC50) > 10 nM Positive ROR1 expression (ROR1+++/++)
Method Description
Ntera-2 cell at 625 cells/25 pL were seeded in a 384-well plat. ADCs were formulated at 2x starting concentration. Filter sterilized samples were serial diluted (1:3) under sterile conditions and added onto cells in triplicates. For cell viability measurement, 30 microliter of Cell Titer-Glo@ reagent (Promega Corp, Madison, WI) was added into each well, and plates processed as per product instructions.

   Click to Show/Hide
In Vitro Model Embryonal carcinoma Ntera-2 cells CVCL_0034
Experiment 2 Reporting the Activity Date of This ADC [9]
Efficacy Data Half Maximal Effective Concentration (EC50) > 10 nM Negative ROR1 expression (ROR1-)
Method Description
MCF-7 cells at 625 cells/25 pL were seeded in a 384-well plat. ADCs were formulated at 2x starting concentration. Filter sterilized samples were serial diluted (1:3) under sterile conditions and added onto cells in triplicates. For cell viability measurement, 30 microliter of Cell Titer-Glo@ reagent (Promega Corp, Madison, WI) was added into each well, and plates processed as per product instructions.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
ZA202500202A D04-F404-LP26 [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [9]
Efficacy Data Half Maximal Effective Concentration (EC50) > 10 nM Positive ROR1 expression (ROR1+++/++)
Method Description
Ntera-2 cell at 625 cells/25 pL were seeded in a 384-well plat. ADCs were formulated at 2x starting concentration. Filter sterilized samples were serial diluted (1:3) under sterile conditions and added onto cells in triplicates. For cell viability measurement, 30 microliter of Cell Titer-Glo@ reagent (Promega Corp, Madison, WI) was added into each well, and plates processed as per product instructions.

   Click to Show/Hide
In Vitro Model Embryonal carcinoma Ntera-2 cells CVCL_0034
Experiment 2 Reporting the Activity Date of This ADC [9]
Efficacy Data Half Maximal Effective Concentration (EC50) > 10 nM Negative ROR1 expression (ROR1-)
Method Description
MCF-7 cells at 625 cells/25 pL were seeded in a 384-well plat. ADCs were formulated at 2x starting concentration. Filter sterilized samples were serial diluted (1:3) under sterile conditions and added onto cells in triplicates. For cell viability measurement, 30 microliter of Cell Titer-Glo@ reagent (Promega Corp, Madison, WI) was added into each well, and plates processed as per product instructions.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
ZA202500202A D04-F404-LP28 [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [9]
Efficacy Data Half Maximal Effective Concentration (EC50) > 10 nM Positive ROR1 expression (ROR1+++/++)
Method Description
Ntera-2 cell at 625 cells/25 pL were seeded in a 384-well plat. ADCs were formulated at 2x starting concentration. Filter sterilized samples were serial diluted (1:3) under sterile conditions and added onto cells in triplicates. For cell viability measurement, 30 microliter of Cell Titer-Glo@ reagent (Promega Corp, Madison, WI) was added into each well, and plates processed as per product instructions.

   Click to Show/Hide
In Vitro Model Embryonal carcinoma Ntera-2 cells CVCL_0034
Experiment 2 Reporting the Activity Date of This ADC [9]
Efficacy Data Half Maximal Effective Concentration (EC50) > 10 nM Negative ROR1 expression (ROR1-)
Method Description
MCF-7 cells at 625 cells/25 pL were seeded in a 384-well plat. ADCs were formulated at 2x starting concentration. Filter sterilized samples were serial diluted (1:3) under sterile conditions and added onto cells in triplicates. For cell viability measurement, 30 microliter of Cell Titer-Glo@ reagent (Promega Corp, Madison, WI) was added into each well, and plates processed as per product instructions.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
References
Ref 1 Clinical Trial of SOT102 Antibody Drug Conjugate in Patients With Advanced Gastric and Pancreatic Adenocarcinoma
Ref 2 NBE-002 in Patients With Advanced Solid Tumors
Ref 3 A Multicentric Phase 1/2 Trial to Evaluate the Safety and Efficacy of SOT102 as Monotherapy and in Combination With Standard of Care Treatment in Patients With Gastric and Pancreatic Adenocarcinoma, NCT05525286
Ref 4 Evaluation of PNU-159682 antibody drug conjugates (ADCs). Bioorg Med Chem Lett. 2020 Dec 15;30(24):127640. doi: 10.1016/j.bmcl.2020.127640. Epub 2020 Oct 28.
Ref 5 Novel b7-h3 binding molecules, antibody drug conjugates thereof and methods of use thereof; 2017-10-19.
Ref 6 Highly Potent, Anthracycline-based Antibody-Drug Conjugates Generated by Enzymatic, Site-specific Conjugation. Mol Cancer Ther. 2017 May;16(5):879-892.
Ref 7 The ROR1 antibody-drug conjugate huXBR1-402-G5-PNU effectively targets ROR1+ leukemia. Blood Adv. 2021 Aug 24;5(16):3152-3162.
Ref 8 Binding protein drug conjugates comprising anthracycline derivatives; 2016-06-30.
Ref 9 Anti-ROR1 antibodies and antibody conjugates, compositions comprising Anti-ROR1 antibodies or antibody conjugates, and methods of making and using Anti-ROR1 antibodies and antibody conjugates