Antibody Information

General Information of This Antibody
Antibody ID
ANTI0DFWLJ
Antibody Name
A52
Organization
EXELIXIS, INC.
Synonyms
anti-IL13Ra2 antibody A52
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Antibody Type
Monoclonal antibody (mAb)
Antibody Subtype
Humanized lgG
Antigen Name
Interleukin-13 receptor subunit alpha-2 (IL13RA2)
  Antigen Info 
Click to Show/Hide the Sequence Information of This Antibody
Heavy Chain Sequence
QMQLVQSGTEVKKPGASVTVSCKASGYTFTGYYVDWVRQAPGQGLEWMGWINPYSGGTSY
AQRFQGRVTMTRDTSVSTAYMELSRLRSDDTAVYYCARGGQQLARRWFDPWGQGTLVTVS
SASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQS
SGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSCDKTHTCPPCPAPELLG
GPSVFLFPPKPKDTLMISRTPEVTCVVvDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQY
NSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRE
EMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSR
WQQGNVFSCSVMHEALHNHYTQKSLSLSPGK
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Heavy Chain Varible Domain
QMQLVQSGTEVKKPGASVTVSCKASGYTFTGYYVDWVRQAPGQGLEWMGWINPYSGGTSY
AQRFQGRVTMTRDTSVSTAYMELSRLRSDDTAVYYCARGGQQLARRWFDPWGQGTLVTVS
S
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Heavy Chain Hinge Region
ASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSS
GLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSCDKTHTCPPCPAPELLGG
PSVFLFPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNS
TYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSREEM
TKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQ
QGNVFSCSVMHEALHNHYTQKSLSLSPGK
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Light Chain Sequence
AIQLTQSPSSLSASVGDRVTITCRASQGIGNYLAWYQQKPGKIPKLLIYAASTLQSGVPS
RFSGSGSGTDFTLTISSLQPEDVATYYCQNYNSVPFTFGPGTKVEIKRTVAAPSVFIFPP
SDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLT
LSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
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Light Chain Varible Domain
AIQLTQSPSSLSASVGDRVTITCRASQGIGNYLAWYQQKPGKIPKLLIYAASTLQSGVPS
RFSGSGSGTDFTLTISSLQPEDVATYYCQNYNSVPFTFGPGTKVEIK
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Light Chain Constant Domain
RTVAAPSVFIFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQD
SKDSTYSLSSTLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
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The Activity Data of This Antibody
Antibody Activity Information 1 [1]
the MFI (geometric mean) signal
≈40000-50000
a.u.
Human HEK 293 cells CVCL_0045 
Antigen Expression Positive IL13Ra2 expression (IL13Ra2+++/++)
Antibody Function FACS was used to evaluate the binding profiles of cells expressing IL13Ra2.
Antibody Antigen Binding Assay FACS was used to evaluate the binding profiles of cells expressing IL13Ra2. The samples were then read by flow cytometry and the MFI (geometric mean) signal was calculated.
Antibody Activity Information 2 [1]
the MFI (geometric mean) signal
≈40000-50000
a.u.
A-375 cells CVCL_0132 
Antigen Expression Positive IL13Ra2 expression (IL13Ra2+++/++)
Antibody Function FACS was used to evaluate the binding profiles of cells expressing IL13Ra2.
Antibody Antigen Binding Assay FACS was used to evaluate the binding profiles of cells expressing IL13Ra2. The samples were then read by flow cytometry and the MFI (geometric mean) signal was calculated.
Antibody Activity Information 3 [1]
Half Maximal Effective Concentration (EC50)
0.2303
nM
U266 (CD38-) cells . 
Antigen Expression High IL13Ra2 expression (IL13Ra2 +++)
Antibody Function LISA was performed to assess the binding profiles of the ADCs produced as described above and their parental antibodies to human IL13Ra2-His protein.
Antibody Antigen Binding Assay LISA was performed to assess the binding profiles of the ADCs produced as described above and their parental antibodies to human IL13Ra2-His protein.
Each Antibody-drug Conjugate Related to This Antibody
Full Information of The Activity Data of The ADC(s) Related to This Antibody
wO2025019776A2ADC 52-8 [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 [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
66.60%
Positive IL13Ra2 expression (IL13Ra2+++/++)
Method Description
Each female BALB/c Nude mouse was inoculated subcutaneously in the right upper/lower flank region with 1x10 7of H2228 tumor cells (an NSCLC cell line having an IL13Ra2 copy number of about 2,000)in 0.1 mL of PBS mixed with MATRIGELR (1:1)for tumor development.When the mean tumor size reached about 80-150 mm 3,mice were randomized into respective treatment groups (10 mice per group)and received intravenous injections of vehicle or a single dose of the tested ADCs at 10 mg/kg on Day 1. Body weights and tumor volumes were measured twice per week until the end of the study (Day 48).

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In Vivo Model CDX Model-H2228
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
83.40%
Positive IL13Ra2 expression (IL13Ra2+++/++)
Method Description
Each female BALB/c Nude mouse was inoculated subcutaneously in the right upper flank region with 0.5x10 6of SK-MES-1 tumor cells (a non-small cell lung cancer (NSCLC)cell line having an IL13Ra2 copy number of about 4x104)in 0.1 mL of PBS for tumor development.When the mean tumor size reached about 80-150 mm 3,mice were randomized into respective treatment groups (10 mice per group)and received intravenous injections of PBS vehicle or a single dose of the tested ADCs at 10 mg/kg on Day 1. The end of the study was day 49.

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In Vivo Model CDX Model-SK-MES-1
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 [1]
Efficacy Data the MFI (geometric mean) signal ≈ 30000-40000 . Positive hIL13Ra2 expression (hIL13Ra2+++/++)
Method Description
FACS was used to evaluate the binding profiles of HEK293 cells engineered to express IL13Ra2 (HEK293-IL13Ra2) cells expressing IL13Ra2. The samples were then read by flow cytometry and the MFI (geometric mean) signal was calculated.
In Vitro Model Normal HEK293 cells CVCL_0045
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data the MFI (geometric mean) signal ≈ 40000-50000 . Positive hIL13Ra2 expression (hIL13Ra2+++/++)
Method Description
FACS was used to evaluate the binding profiles of A375 cells expressing IL13Ra2. The samples were then read by flow cytometry and the MFI (geometric mean) signal was calculated.
In Vitro Model Amelanotic melanoma A375 cells CVCL_0132
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
2 nM
High hIL13Ra2 expression (hIL13Ra2 +++)
Method Description
The cytotoxic activity of ADC 52-8 was determined against cancer cell lines A375.FITC and anti-Hen egg-white lysozyme isotype control antibody (HEWL)conjugated to the same linker payloads.
In Vitro Model Amelanotic melanoma A375 cells CVCL_0132
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 100 nM Positive hIL13Ra2 expression (hIL13Ra2+++/++)
Method Description
The cytotoxic activity of ADC 52-8 was determined against cancer cell lines H1792.FITC and anti-Hen egg-white lysozyme isotype control antibody (HEWL)conjugated to the same linker payloads.
In Vitro Model Lung adenocarcinoma H1792 cells CVCL_1495
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 100 nM Positive hIL13Ra2 expression (hIL13Ra2+++/++)
Method Description
The cytotoxic activity of ADC 52-8 was determined against cancer cell lines H2228.FITC and anti-Hen egg-white lysozyme isotype control antibody (HEWL)conjugated to the same linker payloads.
In Vitro Model Lung adenocarcinoma H2228 cells CVCL_1543
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 100 nM Positive hIL13Ra2 expression (hIL13Ra2+++/++)
Method Description
The cytotoxic activity of ADC 52-8 was determined against cancer cell lines SK-MES-1.FITC and anti-Hen egg-white lysozyme isotype control antibody (HEWL)conjugated to the same linker payloads.
In Vitro Model Lung squamous cell carcinoma SK-MES-1 cells CVCL_0630
wO2025019776A2ADC 52-2 [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.01 nM
High hIL13Ra2 expression (hIL13Ra2 +++)
Method Description
The cytotoxic activity of ADC 52-2 was determined against cancer cell lines A375.FITC and anti-Hen egg-white lysozyme isotype control antibody (HEWL)conjugated to the same linker payloads.
In Vitro Model Amelanotic melanoma A375 cells CVCL_0132
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.02-0.03 nM
Positive hIL13Ra2 expression (hIL13Ra2+++/++)
Method Description
The cytotoxic activity of ADC 52-2 was determined against cancer cell lines H1792.FITC and anti-Hen egg-white lysozyme isotype control antibody (HEWL)conjugated to the same linker payloads.
In Vitro Model Lung adenocarcinoma H1792 cells CVCL_1495
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.04-0.08 nM
Positive hIL13Ra2 expression (hIL13Ra2+++/++)
Method Description
The cytotoxic activity of ADC 52-2 was determined against cancer cell lines H2228.FITC and anti-Hen egg-white lysozyme isotype control antibody (HEWL)conjugated to the same linker payloads.
In Vitro Model Lung adenocarcinoma H2228 cells CVCL_1543
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
3-63 nM
Positive hIL13Ra2 expression (hIL13Ra2+++/++)
Method Description
The cytotoxic activity of ADC 52-2 was determined against cancer cell lines SK-MES-1.FITC and anti-Hen egg-white lysozyme isotype control antibody (HEWL)conjugated to the same linker payloads.
In Vitro Model Lung squamous cell carcinoma SK-MES-1 cells CVCL_0630
References
Ref 1 Interleukin-13 receptor subunit alpha-2 antibody-drug conjugates and uses thereof