General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0WJWEG
ADC Name
AGS67E
Synonyms
AGS67E
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Organization
Agensys (Top20 MNC) (Originator)
Drug Status
Phase 1 (discontinued)
Drug-to-Antibody Ratio
3.7
Structure
Antibody Name
AGS67C
 Antibody Info 
Antigen Name
Leukocyte antigen CD37 (CD37)
 Antigen Info 
Payload Name
MMAE
 Payload Info 
Therapeutic Target
Microtubule (MT)
 Target Info 
Linker Name
Mc-Val-Cit-PABC
 Linker Info 
Conjugate Type
Random Cysteines
Combination Type
vedotin
The indication landscape of This ADC(2027 Update)
The clinical trial pipeline of This ADC(2027 Update)
Indication Phase 1 Phase 1/2 Phase 2 Phase 2/3 Phase 3 New Drug Application Approved
Acute myeloid leukaemia
1 Trials
Trial ID
NCT02610062
Unspecific hematological malignancies
1 Trials
Trial ID
NCT02175433
General Information of The Activity Data Related to This ADC
Identified from the Human Clinical Data
Click To Hide/Show 4 Activity Data Related to This Level
Standard Type NCT Number Clinical Status Clinical Trial Description
Objective Response Rate (ORR)  NCT02175433
Phase 1
A phase 1 study evaluating safety, tolerability, and pharmacokinetics of escalating doses of AGS67E given as monotherapy in subjects with refractory or relapsed lymphoid malignancies.
Undisclosed  NCT02610062
Phase 1
A phase 1 study evaluating safety, tolerability, and pharmacokinetics of escalating doses of AGS67E given as monotherapy in subjects with acute myeloid leukemia (AML).
Undisclosed  NCT02610062
PHASE1
A Phase 1 Study Evaluating Safety, Tolerability, and Pharmacokinetics of Escalating Doses of AGS67E Given as Monotherapy in Subjects With Acute Myeloid Leukemia (AML)
Undisclosed  NCT02175433
PHASE1
A Phase 1 Study Evaluating Safety, Tolerability, and Pharmacokinetics of Escalating Doses of AGS67E Given as Monotherapy in Subjects With Refractory or Relapsed Lymphoid Malignancies
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 22 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
0
%
HEL 92.1.7 cells
Erythroleukemia
Tumor Growth Inhibition value (TGI) 
27
%
DoHH2 cells
Diffuse large B-cell lymphoma germinal center B-cell type
Tumor Growth Inhibition value (TGI) 
31
%
WSU-DLCL2 cells
Diffuse large B-cell lymphoma
Tumor Growth Inhibition value (TGI) 
41
%
KG-1 cells
Adult acute myeloid leukemia
Tumor Growth Inhibition value (TGI) 
51
%
Mino cells
Mantle cell lymphoma
Tumor Growth Inhibition value (TGI) 
63
%
Ramos cells
Burkitt lymphoma
Tumor Growth Inhibition value (TGI) 
66
%
DoHH2 cells
Diffuse large B-cell lymphoma germinal center B-cell type
Tumor Growth Inhibition value (TGI) 
69
%
MOLM-13 cells
Adult acute myeloid leukemia
Tumor Growth Inhibition value (TGI) 
86
%
Ramos cells
Burkitt lymphoma
Tumor Growth Inhibition value (TGI) 
92
%
Mino cells
Mantle cell lymphoma
Tumor Growth Inhibition value (TGI) 
95
%
THP-1 cells
Childhood acute monocytic leukemia
Tumor Growth Inhibition value (TGI) 
95
%
DoHH2 cells
Diffuse large B-cell lymphoma germinal center B-cell type
Tumor Growth Inhibition value (TGI) 
96
%
WSU-DLCL2 cells
Diffuse large B-cell lymphoma
Tumor Growth Inhibition value (TGI) 
97
%
Ramos cells
Burkitt lymphoma
Tumor Growth Inhibition value (TGI) 
100
%
MOLM-13 cells
Adult acute myeloid leukemia
Tumor Growth Inhibition value (TGI) 
100
%
MOLM-13 cells
Adult acute myeloid leukemia
Tumor Growth Inhibition value (TGI) 
100
%
MV4-11 cells
Childhood acute monocytic leukemia
Tumor Growth Inhibition value (TGI) 
100
%
MV4-11 cells
Childhood acute monocytic leukemia
Tumor Growth Inhibition value (TGI) 
100
%
MV4-11 cells
Childhood acute monocytic leukemia
Tumor Growth Inhibition value (TGI) 
100
%
JVM-3 cells
B-cell prolymphocytic leukemia
Tumor Growth Inhibition value (TGI) 
100
%
JVM-3 cells
B-cell prolymphocytic leukemia
Tumor Growth Inhibition value (TGI) 
100
%
JVM-3 cells
B-cell prolymphocytic leukemia
Revealed Based on the Cell Line Data
Click To Hide/Show 25 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
0.05±0.03
nM
Ramos cells
Burkitt lymphoma
Half Maximal Inhibitory Concentration (IC50) 
0.07±0.49
nM
Mino cells
Mantle cell lymphoma
Half Maximal Inhibitory Concentration (IC50) 
0.08±0.61
nM
Granta-519 cells
Mantle cell lymphoma
Half Maximal Inhibitory Concentration (IC50) 
0.08±0.02
nM
Daudi cells
Burkitt lymphoma
Half Maximal Inhibitory Concentration (IC50) 
0.13±0.08
nM
THP-1 cells
Childhood acute monocytic leukemia
Half Maximal Inhibitory Concentration (IC50) 
0.23±0.30
nM
SU-DHL-4 cells
Diffuse large B-cell lymphoma
Half Maximal Inhibitory Concentration (IC50) 
0.50±0.72
nM
JVM-3 cells
B-cell prolymphocytic leukemia
Half Maximal Inhibitory Concentration (IC50) 
0.71±0.20
nM
SKM-1 cells
Acute myeloid leukemia
Half Maximal Inhibitory Concentration (IC50) 
0.98±1.10
nM
DoHH2 cells
Diffuse large B-cell lymphoma germinal center B-cell type
Half Maximal Inhibitory Concentration (IC50) 
1.10±0.60
nM
OCI-AML-2 cells
Adult acute myeloid leukemia
Half Maximal Inhibitory Concentration (IC50) 
1.20±0.90
nM
MV4-11 cells
Childhood acute monocytic leukemia
Half Maximal Inhibitory Concentration (IC50) 
1.30±0.50
nM
MOLM-13 cells
Adult acute myeloid leukemia
Half Maximal Inhibitory Concentration (IC50) 
3.50±0.70
nM
Kasumi-1 cells
Myeloid leukemia with maturation
Half Maximal Inhibitory Concentration (IC50) 
5.70±1.60
nM
BDCM cells
Acute myeloid leukemia
Half Maximal Inhibitory Concentration (IC50) 
19.70±3.00
nM
WSU-DLCL2 cells
Diffuse large B-cell lymphoma
Half Maximal Inhibitory Concentration (IC50) 
> 10
uM
MOLT-4 cells
Adult T acute lymphoblastic leukemia
Half Maximal Inhibitory Concentration (IC50) 
> 10
uM
HEL 92.1 cells
Acute erythroid leukemia
Half Maximal Inhibitory Concentration (IC50) 
> 10
uM
TF-1a cells
Acute erythroid leukemia
Half Maximal Inhibitory Concentration (IC50) 
> 10
uM
CMK cells
Down syndrome
Half Maximal Inhibitory Concentration (IC50) 
> 10
uM
KG-1 cells
Adult acute myeloid leukemia
Half Maximal Inhibitory Concentration (IC50) 
> 10
uM
UT-7 cells
Adult acute megakaryoblastic leukemia
Half Maximal Inhibitory Concentration (IC50) 
> 10
uM
HL-60 cells
Adult acute myeloid leukemia
Half Maximal Inhibitory Concentration (IC50) 
> 10
uM
EoL-1 cells
Chronic eosinophilic leukemia
Half Maximal Inhibitory Concentration (IC50) 
> 10
uM
PL-21 cells
Acute myeloid leukemia
Half Maximal Inhibitory Concentration (IC50) 
> 10
uM
REC-1 cells
Mantle cell lymphoma
Full List of Activity Data of This Antibody-drug Conjugate
Identified from the Human Clinical Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Objective Response Rate (ORR) 24% Low CD37 expression (CD37+; CD37 MFI ratio=82)
Patients Enrolled
Relapsed / refractory non Hodgkin lymphomas (NHLs) and chronic lymphocytic leukemia (CLL).
Administration Dosage
Administered intravenously (IV) once every 3 weeks (Q3 weeks) until disease progression or unacceptable toxicity.
Related Clinical Trial
NCT Number NCT02175433  Clinical Status Phase 1
Clinical Description A phase 1 study evaluating safety, tolerability, and pharmacokinetics of escalating doses of AGS67E given as monotherapy in subjects with refractory or relapsed lymphoid malignancies.
Experiment 2 Reporting the Activity Date of This ADC [2]
Related Clinical Trial
NCT Number NCT02610062  Clinical Status Phase 1
Clinical Description A phase 1 study evaluating safety, tolerability, and pharmacokinetics of escalating doses of AGS67E given as monotherapy in subjects with acute myeloid leukemia (AML).
Experiment 3 Reporting the Activity Date of This ADC [4]
Patients Enrolled
Site-specific conjugation through the engineered C-terminal cysteine
Administration Dosage
Participants will receive 1.2, 1.8, 2.4, 0.6, 0.9 mg/kg of AGS67E as an intravenous infusion once every three weeks (Q3).
Related Clinical Trial
NCT Number NCT02610062  Clinical Status PHASE1
Clinical Description A Phase 1 Study Evaluating Safety, Tolerability, and Pharmacokinetics of Escalating Doses of AGS67E Given as Monotherapy in Subjects With Acute Myeloid Leukemia (AML)
Primary Endpoint
This clinical trial evaluates AGS67E, an antibody-drug conjugate (ADC), in acute myeloid leukemia (AML) patients, focusing on safety (adverse events, anti-drug antibodies), pharmacokinetics (Cmax, AUC, half-life of AGS67E components), and efficacy (complete remission rate, response duration). Key inclusion: relapsed/refractory or untreated AML (WHO 2008 criteria), ECOG ≤2, adequate organ function. Exclusion: APL, active GVHD, neuropathy ≥G2, recent chemo (<14 days), uncontrolled infections, or cardiac disease.

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Other Endpoint
The study includes dose escalation (Q3W/weekly) and expansion phases with PK sampling (up to 12 months). Primary endpoints: safety/tolerability (AEs, ADA incidence) and PK parameters (TAb, ADC, MMAE). Secondary endpoints: efficacy (CR/CRc rates, best response). Hydroxyurea is permitted for blast control; P-gp/CYP3A modulators are restricted unless prophylactic.

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Experiment 4 Reporting the Activity Date of This ADC [5]
Patients Enrolled
Site-specific conjugation through unnatural amino acid (pAF 121).
Administration Dosage
Participants will receive 0.05, 0.1, 0.3, 0.6, 0.9, 1.2 milligram per kilogram (mg/kg) AGS67E without growth factor (GF) by intravenous infusion once every three weeks.
Related Clinical Trial
NCT Number NCT02175433  Clinical Status PHASE1
Clinical Description A Phase 1 Study Evaluating Safety, Tolerability, and Pharmacokinetics of Escalating Doses of AGS67E Given as Monotherapy in Subjects With Refractory or Relapsed Lymphoid Malignancies
Primary Endpoint
Safety evaluation included the incidence and severity of adverse events over 34 months, alongside comprehensive pharmacokinetic assessments of total antibody (TAb), antibody-drug conjugate (ADC), and MMAE at defined intervals during escalation and expansion phases, covering key metrics such as CEOI, Cmax, Tmax, AUC, half-life, systemic clearance, and volume of distribution.

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Other Endpoint
Immunogenicity was assessed through Anti-Drug Antibody (ADA) formation against AGS67C/AGS67E, while efficacy endpoints included tumor response rates (CR/PR) and objective response rate (ORR), measured over the 34-month study period.
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 22 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) 0% Low CD37 expression (CD37+; CD37 MFI ratio=82)
Method Description
The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.

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In Vivo Model CD37-expressing Hel 92.1.7 AmL cancer xenograft model
In Vitro Model Erythroleukemia HEL 92.1.7 cells CVCL_2481
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) 27% High CD37 expression (CD37+++; CD37 MFI ratio=580)
Method Description
The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.

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In Vivo Model CD37-expressing DOHH2 FL cancer xenograft model
In Vitro Model Diffuse large B-cell lymphoma germinal center B-cell type DoHH2 cells CVCL_1179
Experiment 3 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) 31% High CD37 expression (CD37+++; CD37 MFI ratio=554)
Method Description
The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.

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In Vivo Model CD37-expressing WSU-DLCL2 DBCL cancer xenograft model
In Vitro Model Diffuse large B-cell lymphoma WSU-DLCL2 cells CVCL_1902
Experiment 4 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) 41% Low CD37 expression (CD37+; CD37 MFI ratio=20)
Method Description
The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.

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In Vivo Model CD37-expressing KG-1 AmL cancer xenograft model
In Vitro Model Adult acute myeloid leukemia KG-1 cells CVCL_0374
Experiment 5 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) 51% High CD37 expression (CD37+++; CD37 MFI ratio=300)
Method Description
The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.

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In Vivo Model CD37-expressing Mino MCL cancer xenograft model
In Vitro Model Mantle cell lymphoma Mino cells CVCL_1872
Experiment 6 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) 63% Moderate CD37 expression (CD37++; CD37 MFI ratio=140)
Method Description
The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.

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In Vivo Model CD37-expressing Ramos-RR-XcL Burkitt lymphoma cancer xenograft model
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
Experiment 7 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) 66% High CD37 expression (CD37+++; CD37 MFI ratio=580)
Method Description
The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.

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In Vivo Model CD37-expressing DOHH2 FL cancer xenograft model
In Vitro Model Diffuse large B-cell lymphoma germinal center B-cell type DoHH2 cells CVCL_1179
Experiment 8 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) 69% Low CD37 expression (CD37+; CD37 MFI ratio=25)
Method Description
The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.

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In Vivo Model CD37-expressing MOLM-13 AmL cancer xenograft model
In Vitro Model Adult acute myeloid leukemia MOLM-13 cells CVCL_2119
Experiment 9 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) 86% Moderate CD37 expression (CD37++; CD37 MFI ratio=140)
Method Description
The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.

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In Vivo Model CD37-expressing Ramos-RR-XcL Burkitt lymphoma cancer xenograft model
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
Experiment 10 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) 92% High CD37 expression (CD37+++; CD37 MFI ratio=300)
Method Description
The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.

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In Vivo Model CD37-expressing Mino MCL cancer xenograft model
In Vitro Model Mantle cell lymphoma Mino cells CVCL_1872
Experiment 11 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) 95% Low CD37 expression (CD37+; CD37 MFI ratio=23)
Method Description
The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.

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In Vivo Model CD37-expressing THP-1 AmL cancer xenograft models
In Vitro Model Childhood acute monocytic leukemia THP-1 cells CVCL_0006
Experiment 12 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) 95% High CD37 expression (CD37+++; CD37 MFI ratio=580)
Method Description
The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.

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In Vivo Model CD37-expressing DOHH2 FL cancer xenograft model
In Vitro Model Diffuse large B-cell lymphoma germinal center B-cell type DoHH2 cells CVCL_1179
Experiment 13 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) 96% High CD37 expression (CD37+++; CD37 MFI ratio=554)
Method Description
The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.

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In Vivo Model CD37-expressing WSU-DLCL2 DBCL cancer xenograft model
In Vitro Model Diffuse large B-cell lymphoma WSU-DLCL2 cells CVCL_1902
Experiment 14 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) 97% Moderate CD37 expression (CD37++; CD37 MFI ratio=140)
Method Description
The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.

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In Vivo Model CD37-expressing Ramos-RR-XcL Burkitt lymphoma cancer xenograft model
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
Experiment 15 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) 100% Low CD37 expression (CD37+; CD37 MFI ratio=25)
Method Description
The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.

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In Vivo Model CD37-expressing MOLM-13 AmL cancer xenograft model
In Vitro Model Adult acute myeloid leukemia MOLM-13 cells CVCL_2119
Experiment 16 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) 100% Low CD37 expression (CD37+; CD37 MFI ratio=25)
Method Description
The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.

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In Vivo Model CD37-expressing MOLM-13 AmL cancer xenograft model
In Vitro Model Adult acute myeloid leukemia MOLM-13 cells CVCL_2119
Experiment 17 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) 100% Low CD37 expression (CD37+; CD37 MFI ratio=22)
Method Description
The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.

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In Vivo Model CD38-expressing MV-411 AmL cancer xenograft model
In Vitro Model Childhood acute monocytic leukemia MV4-11 cells CVCL_0064
Experiment 18 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) 100% Low CD37 expression (CD37+; CD37 MFI ratio=22)
Method Description
The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.

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In Vivo Model CD38-expressing MV-411 AmL cancer xenograft model
In Vitro Model Childhood acute monocytic leukemia MV4-11 cells CVCL_0064
Experiment 19 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) 100% Low CD37 expression (CD37+; CD37 MFI ratio=22)
Method Description
The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.

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In Vivo Model CD38-expressing MV-411 AmL cancer xenograft model
In Vitro Model Childhood acute monocytic leukemia MV4-11 cells CVCL_0064
Experiment 20 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) 100% Moderate CD37 expression (CD37++; CD37 MFI ratio=129)
Method Description
The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.

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In Vivo Model CD38-expressing JVM3 xenograft CLL cancer model
In Vitro Model B-cell prolymphocytic leukemia JVM-3 cells CVCL_1320
Experiment 21 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) 100% Moderate CD37 expression (CD37++; CD37 MFI ratio=129)
Method Description
The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.

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In Vivo Model CD38-expressing JVM3 xenograft CLL cancer model
In Vitro Model B-cell prolymphocytic leukemia JVM-3 cells CVCL_1320
Experiment 22 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) 100% Moderate CD37 expression (CD37++; CD37 MFI ratio=129)
Method Description
The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.

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In Vivo Model CD38-expressing JVM3 xenograft CLL cancer model
In Vitro Model B-cell prolymphocytic leukemia JVM-3 cells CVCL_1320
Revealed Based on the Cell Line Data
Click To Hide/Show 25 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.05±0.03 nM Low CD37 expression (CD37+; CD37 MFI ratio=25)
Method Description
The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).

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In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.07±0.49 nM Low CD37 expression (CD37+; CD37 MFI ratio=18)
Method Description
The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).

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In Vitro Model Mantle cell lymphoma Mino cells CVCL_1872
Experiment 3 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.08±0.61 nM Negative CD37 expression (CD37-; CD37 MFI ratio=3)
Method Description
The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).

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In Vitro Model Mantle cell lymphoma Granta-519 cells CVCL_1818
Experiment 4 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.08±0.02 nM
Method Description
The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).

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In Vitro Model Burkitt lymphoma Daudi cells CVCL_0008
Experiment 5 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.13±0.08 nM High CD37 expression (CD37+++; CD37 MFI ratio=662)
Method Description
The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).

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In Vitro Model Childhood acute monocytic leukemia THP-1 cells CVCL_0006
Experiment 6 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.23±0.30 nM High CD37 expression (CD37+++; CD37 MFI ratio=534)
Method Description
The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).

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In Vitro Model Diffuse large B-cell lymphoma SU-DHL-4 cells CVCL_0539
Experiment 7 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.50±0.72 nM High CD37 expression (CD37+++; CD37 MFI ratio=581)
Method Description
The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).

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In Vitro Model B-cell prolymphocytic leukemia JVM-3 cells CVCL_1320
Experiment 8 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.71±0.20 nM Low CD37 expression (CD37+; CD37 MFI ratio=22)
Method Description
The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).

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In Vitro Model Acute myeloid leukemia SKM-1 cells CVCL_0098
Experiment 9 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.98±1.10 nM Negative CD37 expression (CD37-; CD37 MFI ratio=9)
Method Description
The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).

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In Vitro Model Diffuse large B-cell lymphoma germinal center B-cell type DoHH2 cells CVCL_1179
Experiment 10 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 1.10±0.60 nM Moderate CD37 expression (CD37++; CD37 MFI ratio=129)
Method Description
The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).

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In Vitro Model Adult acute myeloid leukemia OCI-AML-2 cells CVCL_1619
Experiment 11 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 1.20±0.90 nM Negative CD37 expression (CD37-; CD37 MFI ratio=1)
Method Description
The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).

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In Vitro Model Childhood acute monocytic leukemia MV4-11 cells CVCL_0064
Experiment 12 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 1.30±0.50 nM Low CD37 expression (CD37+; CD37 MFI ratio=20)
Method Description
The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).

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In Vitro Model Adult acute myeloid leukemia MOLM-13 cells CVCL_2119
Experiment 13 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 3.50±0.70 nM Low CD37 expression (CD37+; CD37 MFI ratio=11)
Method Description
The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).

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In Vitro Model Myeloid leukemia with maturation Kasumi-1 cells CVCL_0589
Experiment 14 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 5.70±1.60 nM Low CD37 expression (CD37+; CD37 MFI ratio=26)
Method Description
The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).

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In Vitro Model Acute myeloid leukemia BDCM cells CVCL_4613
Experiment 15 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 19.70±3.00 nM High CD37 expression (CD37+++; CD37 MFI ratio=341)
Method Description
The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).

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In Vitro Model Diffuse large B-cell lymphoma WSU-DLCL2 cells CVCL_1902
Experiment 16 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10 uM Low CD37 expression (CD37+; CD37 MFI ratio=23)
Method Description
The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).

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In Vitro Model Adult T acute lymphoblastic leukemia MOLT-4 cells CVCL_0013
Experiment 17 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10 uM Low CD37 expression (CD37+; CD37 MFI ratio=64)
Method Description
The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).

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In Vitro Model Acute erythroid leukemia HEL 92.1 cells CVCL_2481
Experiment 18 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10 uM Low CD37 expression (CD37+; CD37 MFI ratio=10)
Method Description
The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).

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In Vitro Model Acute erythroid leukemia TF-1a cells CVCL_3608
Experiment 19 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10 uM Low CD37 expression (CD37+; CD37 MFI ratio=30)
Method Description
The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).

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In Vitro Model Down syndrome CMK cells CVCL_0216
Experiment 20 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10 uM Negative CD37 expression (CD37-; CD37 MFI ratio=5)
Method Description
The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).

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In Vitro Model Adult acute myeloid leukemia KG-1 cells CVCL_0374
Experiment 21 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10 uM Negative CD37 expression (CD37-; CD37 MFI ratio=4)
Method Description
The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).

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In Vitro Model Adult acute megakaryoblastic leukemia UT-7 cells CVCL_2233
Experiment 22 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10 uM High CD37 expression (CD37+++; CD37 MFI ratio=372)
Method Description
The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).

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In Vitro Model Adult acute myeloid leukemia HL-60 cells CVCL_0002
Experiment 23 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10 uM Low CD37 expression (CD37+; CD37 MFI ratio=39)
Method Description
The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).

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In Vitro Model Chronic eosinophilic leukemia EoL-1 cells CVCL_0258
Experiment 24 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10 uM High CD37 expression (CD37+++; CD37 MFI ratio=554)
Method Description
The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).

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In Vitro Model Acute myeloid leukemia PL-21 cells CVCL_2161
Experiment 25 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10 uM High CD37 expression (CD37+++; CD37 MFI ratio=301)
Method Description
The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).

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In Vitro Model Mantle cell lymphoma REC-1 cells CVCL_1884
References
Ref 1 A phase 1 study of the anti-CD37 antibody-drug conjugate AGS67E in advanced lymphoid malignancies. interim results. Hematol Oncol. 2017 Jun 7;35(S2):supplement 14-17.
Ref 2 A Phase 1 Study Evaluating Safety, Tolerability, and Pharmacokinetics of Escalating Doses of AGS67E Given as Monotherapy in Subjects With Acute Myeloid Leukemia (AML), NCT02610062
Ref 3 AGS67E, an Anti-CD37 Monomethyl Auristatin E Antibody-Drug Conjugate as a Potential Therapeutic for B/T-Cell Malignancies and AML: A New Role for CD37 in AML. Mol Cancer Ther. 2015 Jul;14(7):1650-60.
Ref 4 A Study to Evaluate Safety, Tolerability, and Pharmacokinetics of Escalating Doses of AGS67E Given as Monotherapy in Subjects With Acute Myeloid Leukemia (AML)
Ref 5 A Study to Evaluate Safety, Tolerability, and Pharmacokinetics of Escalating Doses of AGS67E Given as Monotherapy in Subjects With Refractory or Relapsed Lymphoid Malignancies