General Information of This Payload
Payload ID
PAY0ZJMHY
Name
Glucuronyl-monomethyl-auristatin E (MMAU)
Synonyms
Glucuronyl-monomethyl-auristatin E (MMAU)
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Target Microtubule (MT)
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
EGFR-MMAU ADC [Investigative]
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 [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 84.20% Positive EGFR expression (EGFR+++/++)
Method Description
MMAU ADCs (3 mg/kg, intravenously four times at seven day intervals) induces efficient tumor cell killing in cell line-derived models of HSC-2 cells with EGFR expression with high expression.
In Vivo Model HSC-2 CDX model
In Vitro Model Oral cavity squamous cell carcinoma HSC-2 cells CVCL_1287
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 86.30% Positive EGFR expression (EGFR+++/++)
Method Description
MMAU ADCs (10 mg/kg, intravenously four times at seven day intervals) induces efficient tumor cell killing in cell line-derived models of HSC-2 cells with EGFR expression with high expression.
In Vivo Model HSC-2 CDX model
In Vitro Model Oral cavity squamous cell carcinoma HSC-2 cells CVCL_1287
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 [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
25 pM
Low EGFR expression (EGFR+)
Method Description
Cells were seeded in a culture-treated 96-well clear plate and incubated at 37°C under 5% CO2 for 24h. Serially diluted samples (50L) were added to each well and the plate was incubated at 37°C for 72h.
In Vitro Model Non-small cell lung carcinoma NCI-H522 cells CVCL_1567
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
30 pM
High EGFR expression (EGFR+++)
Method Description
Cells were seeded in a culture-treated 96-well clear plate and incubated at 37°C under 5% CO2 for 24h. Serially diluted samples (50L) were added to each well and the plate was incubated at 37°C for 72h.
In Vitro Model Breast ductal carcinoma HCC1954 cells CVCL_1259
GLK-33 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 8 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.14 nM
Positive CD33 expression (CD33+++/++)
Method Description
GLK-33 exhibited remarkable efficacy in reducing cell viability within CD33-positive leukemia cell lines.
In Vitro Model Childhood acute monocytic leukemia MV4-11 cells CVCL_0064
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.21 nM
Positive CD33 expression (CD33+++/++)
Method Description
GLK-33 exhibited remarkable efficacy in reducing cell viability within CD33-positive leukemia cell lines.
In Vitro Model Adult acute myeloid leukemia MOLM-13 cells CVCL_2119
Experiment 3 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.24 nM
Positive CD33 expression (CD33+++/++)
Method Description
GLK-33 exhibited remarkable efficacy in reducing cell viability within CD33-positive leukemia cell lines.
In Vitro Model Acute myeloblastic leukemia with maturation, Adult acute myeloid leukemia with maturation HL60 cells CVCL_0002
Experiment 4 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
1.4 nM
Positive CD33 expression (CD33+++/++)
Method Description
GLK-33 exhibited remarkable efficacy in reducing cell viability within CD33-positive leukemia cell lines.
In Vitro Model Adult acute myeloid leukemia KG-1 cells CVCL_0374
Experiment 5 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
2.7 nM
Positive CD33 expression (CD33+++/++)
Method Description
GLK-33 exhibited remarkable efficacy in reducing cell viability within CD33-positive leukemia cell lines.
In Vitro Model Acute myeloid leukemia OCI-M1 cells CVCL_2149
Experiment 6 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
725 nM
Positive CD33 expression (CD33+++/++)
Method Description
GLK-33 exhibited remarkable efficacy in reducing cell viability within CD33-positive leukemia cell lines.
In Vitro Model Chronic myelogenous leukemia K-562 cells CVCL_0004
Experiment 7 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 1000 nM Negative CD33 expression (CD33-)
Method Description
GLK-33 exhibited remarkable efficacy in reducing cell viability within CD33-positive leukemia cell lines.
In Vitro Model Burkitt lymphoma Daudi cells CVCL_0008
Experiment 8 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 1000 nM Negative CD33 expression (CD33-)
Method Description
GLK-33 exhibited remarkable efficacy in reducing cell viability within CD33-positive leukemia cell lines.
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
References
Ref 1 Hydrophilic Auristatin Glycoside Payload Enables Improved Antibody-Drug Conjugate Efficacy and Biocompatibility. Antibodies (Basel). 2018 Mar 22;7(2):15. doi: 10.3390/antib7020015.
Ref 2 Targeting CD33+ Acute Myeloid Leukemia with GLK-33, a Lintuzumab-Auristatin Conjugate with a Wide Therapeutic Window