Payload Information

General Information of This Payload
Payload ID
PAY0QCAJM
Name
Saporin
Synonyms
Ber-H2/saporin; D0A9QL
   Click to Show/Hide
Target(s) Microtubule (MT)
 Target Info 
Structure
Formula
C46H42Cl2N2O4Sr
Isosmiles
CC1(CC2=C(C(=C(N2C1)CC(=O)[O-])C3=CC=C(C=C3)Cl)C4=CC=CC=C4)C.CC1(CC2=C(C(=C(N2C1)CC(=O)[O-])C3=CC=C(C=C3)Cl)C4=CC=CC=C4)C.[Sr+2]
PubChem CID
11542423
InChI
InChI=1S/2C23H22ClNO2.Sr/c2*1-23(2)13-19-22(15-6-4-3-5-7-15)21(16-8-10-17(24)11-9-16)18(12-20(26)27)25(19)14-23;/h2*3-11H,12-14H2,1-2H3,(H,26,27);/q;;+2/p-2
InChIKey
LRDCMWNTZTVTAN-UHFFFAOYSA-L
IUPAC Name
strontium;2-[2-(4-chlorophenyl)-6,6-dimethyl-1-phenyl-5,7-dihydropyrrolizin-3-yl]acetate
Pharmaceutical Properties
Molecule Weight
845.4
Polar area
90.1
Complexity
531
xlogp Value
.
Heavy Count
55
Rot Bonds
6
Hbond acc
4
Hbond Donor
0
The activity data of This Payload
Standard Type Value Units Cell line Disease Model Cell line ID Reference
Half Maximal Inhibitory Concentration (IC50) >1.00E-08 M
Jurkat cells
T acute lymphoblastic leukemia
CVCL_0065 
[1]
Half Maximal Inhibitory Concentration (IC50) >1.00E-08 M
Raji cells
EBV-related Burkitt lymphoma
CVCL_0511 
[1]
Half Maximal Inhibitory Concentration (IC50) >1.00E-08 M
MOLT-4 cells
Adult T acute lymphoblastic leukemia
CVCL_0013 
[1]
Half Maximal Inhibitory Concentration (IC50) >1.00E-08 M
D430B cells
Lymphoma
Undisclosed [1]
Cell survival rate 50 %
HCT 116 cells
Colon cancer
CVCL_0291 
[2]
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
HB22.7-SAP [Investigative]
 ADC Info 
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 10 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 2.67% (Day 18) Positive CD22 expression (CD22+++/++)
Method Description
Free hB22.7 (0.6 mg/kg) plus free sap (0.36 mg/kg).
In Vivo Model Raji NhLcells xenograft model
In Vitro Model EBV-related Burkitt lymphoma Raji cells CVCL_0511
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 13.33% (Day 18) Positive CD22 expression (CD22+++/++)
Method Description
HB22.7-sap (1 mg/kg).
In Vivo Model Raji NhLcells xenograft model
In Vitro Model EBV-related Burkitt lymphoma Raji cells CVCL_0511
Experiment 3 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI)
100.00%
High CD22 expression (CD22+++)
Method Description
Nude mice were subcutaneously injected with 5 x 106 Raji cells. Twenty-four h later, designated as day 0, mice were randomly separated into three treatment groups (n = 810 per group) consisting of PBS, free HB22.7 (0.6 mg/kg) plus free SAP (0.36 mg/kg) and HB22.7-SAP (1 mg/kg).
In Vitro Model EBV-related Burkitt lymphoma Raji cells CVCL_0511
Experiment 4 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.00 ng/mL
Positive CD22 expression (CD22+++/++)
Method Description
The inhibitory activity of HB22.7-sap exerted a potent cytotoxic effect against all CD22+ NHL cell lines.
In Vitro Model Diffuse large B-cell lymphoma germinal center B-cell type DoHH2 cells CVCL_1179
Experiment 5 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
4.70 ng/mL
Positive CD22 expression (CD22+++/++)
Method Description
The inhibitory activity of HB22.7-sap exerted a potent cytotoxic effect against all CD22+ NHL cell lines.
In Vitro Model EBV-related Burkitt lymphoma Raji cells CVCL_0511
Experiment 6 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
7.60 ng/mL
Positive CD22 expression (CD22+++/++)
Method Description
The inhibitory activity of HB22.7-sap exerted a potent cytotoxic effect against all CD22+ NHL cell lines.
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)
8.40 ng/mL
Positive CD22 expression (CD22+++/++)
Method Description
The inhibitory activity of HB22.7-sap exerted a potent cytotoxic effect against all CD22+ NHL cell lines.
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
Experiment 8 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 250.00 ng/mL Positive CD22 expression (CD22+++/++)
Method Description
The inhibitory activity of HB22.7-sap exerted a potent cytotoxic effect against all CD22+ NHL cell lines.
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
Experiment 9 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 250.00 ng/mL Negative CD22 expression (CC22-)
Method Description
The inhibitory activity of HB22.7-sap exerted a potent cytotoxic effect against all CD22+ NHL cell lines.
In Vitro Model T acute lymphoblastic leukemia Jurkat cells CVCL_0065
Experiment 10 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
519.00 ng/mL
Positive CD22 expression (CD22+++/++)
Method Description
The inhibitory activity of HB22.7-sap exerted a potent cytotoxic effect against all CD22+ NHL cell lines.
In Vitro Model Mantle cell lymphoma Granta-519 cells CVCL_1818
Revealed Based on the Cell Line Data
Click To Hide/Show 6 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.00 ng/mL
Moderate CD22 expression (CD22++)
Method Description
The in vitro cytotoxicity of HB22.7-SAP was evaluated using an MTS assay. Cells were seeded in 96-well plates at a density of 1 x104 cells/well in 90 uL media. HB22.7-SAP was serially diluted with media and 10 L of each dilution was added to the appropriate well and incubated continuously for 72 h.
In Vitro Model Diffuse large B-cell lymphoma SU-DHL-4 cells CVCL_0539
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.60 ng/mL
Moderate CD22 expression (CD22++)
Method Description
The in vitro cytotoxicity of HB22.7-SAP was evaluated using an MTS assay. Cells were seeded in 96-well plates at a density of 1 1 x104 cells/well in 90 uL media. HB22.7-SAP was serially diluted with media and 10 L of each dilution was added to the appropriate well and incubated continuously for 72 h.
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 Half Maximal Inhibitory Concentration (IC50)
4.70 ng/mL
High CD22 expression (CD22+++)
Method Description
The in vitro cytotoxicity of HB22.7-SAP was evaluated using an MTS assay. Cells were seeded in 96-well plates at a density of 1x104 cells/well in 90 L media. HB22.7-SAP was serially diluted with media and 10 L of each dilution was added to the appropriate well and incubated continuously for 72 h.
In Vitro Model EBV-related Burkitt lymphoma Raji cells CVCL_0511
Experiment 4 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
7.60 ng/mL
Moderate CD22 expression (CD22++)
Method Description
The in vitro cytotoxicity of HB22.7-SAP was evaluated using an MTS assay. Cells were seeded in 96-well plates at a density of 1x104 cells/well in 90 L media. HB22.7-SAP was serially diluted with media and 10 L of each dilution was added to the appropriate well and incubated continuously for 72 h.
In Vitro Model Mantle cell lymphoma Granta-519 cells CVCL_1818
Experiment 5 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
8.40 ng/mL
High CD22 expression (CD22+++)
Method Description
The in vitro cytotoxicity of HB22.7-SAP was evaluated using an MTS assay. Cells were seeded in 96-well plates at a density of 1x104 cells/well in 90 L media. HB22.7-SAP was serially diluted with media and 10 L of each dilution was added to the appropriate well and incubated continuously for 72 h.
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
Experiment 6 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 2500.00 ng/mL Negative CD22 expression (CC22-)
Method Description
The in vitro cytotoxicity of HB22.7-SAP was evaluated using an MTS assay. Cells were seeded in 96-well plates at a density of 1 x104 cells/well in 90 uL media. HB22.7-SAP was serially diluted with media and 10 uL of each dilution was added to the appropriate well and incubated continuously for 72 h.
In Vitro Model T acute lymphoblastic leukemia Jurkat cells CVCL_0065
ITcetuximab [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 [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 85.00% (Day 16) Positive EGFR expression (EGFR +++/++)
Method Description
Mice were injected intraperitoneally with 3 mg/kg of ITcetuximab, and 2days later,2 h after the administration of NPe6 (5 mg/kg) via the tail vein, the tumors were irradiated with a 664 nm laser at a dose of 30 J/cm2 from the diode laser unit.
In Vivo Model A549 CDX model
In Vitro Model Lung adenocarcinoma A-549 cells CVCL_0023
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.36 nM
High EGFR expression (EGFR +++)
Method Description
Cancer cell lines were incubated with compounds for 72 h. IC50 was evaluated from the sigmoid curve obtained using the curvefitting tool of the ImageJ software.
In Vitro Model Skin squamous cell carcinoma A-431 cells CVCL_0037
Experiment 2 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.77 nM
Positive EGFR expression (EGFR +++/++)
Method Description
Cancer cell lines were incubated with compounds for 72 h. IC50 was evaluated from the sigmoid curve obtained using the curvefitting tool of the ImageJ software.
In Vitro Model Lung adenocarcinoma A-549 cells CVCL_0023
Experiment 3 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10.00 nM Low EGFR expression (EGFR +)
Method Description
Cancer cell lines were incubated with compounds for 72 h. IC50 was evaluated from the sigmoid curve obtained using the curvefitting tool of the ImageJ software.
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
5E3-Saporin ADC [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
5.90 pM
Positive SEMA4A expression (SEMA4A +++/++)
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 Plasma cell myeloma NCI-H929 cells CVCL_1600
Experiment 2 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
10.60 pM
Positive SEMA4A expression (SEMA4A +++/++)
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 Plasma cell myeloma MM1.S cells CVCL_8792
Experiment 3 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 100 nM Negative SEMA4A expression (SEMA4A -)
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 Chronic myeloid leukemia K562 cells CVCL_0004
Anti-alpha10-SAP [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [6]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
69.00 nM
Positive ITGA10 expression (ITGA10+++/++)
Method Description
Viability analysis of U3046 mg GBM cells after treatment with increasing concentration of anti-alpha10-SAP or anti-ctrl-SAP for 96 h.
In Vitro Model Glioblastoma U3046MG cells CVCL_IR78
References
Ref 1 High in Vitro Anti-Tumor Efficacy of Dimeric Rituximab/Saporin-S6 Immunotoxin. Toxins (Basel). 2016 Jun 21;8(6):192.
Ref 2 Targeted delivery and enhanced cytotoxicity of cetuximab-saporin by photochemical internalization in EGFR-positive cancer cells. Mol Pharm. 2007 Mar-Apr;4(2):241-51.
Ref 3 Efficacy and toxicity of a CD22-targeted antibody-saporin conjugate in a xenograft model of non-Hodgkin's lymphoma. Oncoimmunology. 2012 Dec 1;1(9):1469-1475.
Ref 4 Development of a new minimally invasive phototherapy for lung cancer using antibody-toxin conjugate. Thorac Cancer. 2023 Mar;14(7):645-653. doi: 10.1111/1759-7714.14776. Epub 2023 Jan 19.
Ref 5 Unbiased cell surface proteomics identifies SEMA4A as an effective immunotherapy target for myeloma. Blood. 2022 Apr 21;139(16):2471-2482. doi: 10.1182/blood.2021015161.
Ref 6 Integrin 10, a Novel Therapeutic Target in Glioblastoma, Regulates Cell Migration, Proliferation, and Survival. Cancers (Basel). 2019 Apr 25;11(4):587. doi: 10.3390/cancers11040587.

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