General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0YVPYT
ADC Name
kR1020250008730A 99961.1-MMAE
Synonyms
99961.1-MMAE
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Organization
SANYOU BIOPHARMACEUTICALS CO. LTD. | HANGZHOU ZHONGMEIHUADONG PHARMACEUTICAL CO. LTD.
Drug Status
Investigative
Drug-to-Antibody Ratio
3.8
Structure
Antibody Name
99961.1
 Antibody Info 
Antigen Name
Inactive tyrosine-protein kinase transmembrane receptor ROR1 (ROR1)
 Antigen Info 
Payload Name
Monomethyl auristatin E
 Payload Info 
Therapeutic Target
Microtubule (MT)
 Target Info 
Linker Name
Mc-Val-Cit-PABC
 Linker Info 
Conjugate Type
Random conjugation through reduced inter-chain cysteines.
General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 15 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth lnhibition value (TGl) 
11.08
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
15.9
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
34.6
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
37.81
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
59.22
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
64.31
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
67.66
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
89.35
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
91.74
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
95.77
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
96.6
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
97.86
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
98.21
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
99.2
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
100
%
Undisclosed Undisclosed
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 15 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
11.08%
Method Description
A xenograft model derived from cell lines was established by unilateral subcutaneous injection of 1×10^6 HT-29 cells into female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, 99961.1-MMAE was administered at a dose of 0.4 mg/kg. The treatment was given twice a week for 4 weeks. The tumor inhibition rate was calculated at the end of the experiment.

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In Vivo Model HT-29-xenograft model
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
15.90%
Method Description
A xenograft model derived from cell lines was established by unilateral subcutaneous injection of 1×10^6 HT-29 cells into female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, 99961.1-MMAE was administered at a dose of 2 mg/kg. The treatment was given twice a week for 4 weeks. The tumor inhibition rate was calculated at the end of the experiment.

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In Vivo Model HT-29-xenograft model
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
34.60%
Method Description
A xenograft model derived from cell lines was established by injecting 1×10^7 Jeko cells subcutaneously into the left side of female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, 99961.1-MMAE at doses of 2.5 mg/kg and 3.5 mg/kg was administered on the 15th and 29th days respectively. The tumor inhibition rate was calculated at the end of the experiment.

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In Vivo Model Jeko-1-xenograft model
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
37.81%
Method Description
A xenograft model derived from cell lines was established by unilateral subcutaneous injection of 1×10^6 A549 cells into female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, 99961.1-MMAE was administered at a dose of 10 mg/kg. The treatment was given twice a week for 3 weeks. The tumor inhibition rate was calculated at the end of the experiment.

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In Vivo Model A549-xenograft model
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
59.22%
Method Description
A xenograft model derived from cell lines was established by injecting 1×10^7 Jeko cells subcutaneously into the left side of female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, 99961.1-MMAE was administered at a dose of 2.5 mg/kg. The treatment was given once a week for 3 weeks. The tumor inhibition rate was calculated at the end of the experiment.

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In Vivo Model Jeko-1-xenograft model
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
64.31%
Method Description
A xenograft model derived from cell lines was established by injecting 1×10^7 MDA-MB-468 cells subcutaneously into female BALB/C nude mice. When the tumor volume reached approximately 100 mm^3, 99961.1-MMAE was administered at a dose of 10 mg/kg once. The tumor inhibition rate was calculated at the end of the experiment.
In Vivo Model MDA-MB-468-xenograft model
Experiment 7 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
67.66%
Method Description
A xenograft model derived from the cell line was established by injecting 1×10^6 MDA-MB-231 cells subcutaneously into the left side of female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, B31-H3L3-MMAE was administered at a dose of 5 mg/kg. The treatment was given once a week for 3 weeks. The tumor inhibition rate was calculated at the end of the experiment.

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In Vivo Model MDA-MB-231-xenograft model
Experiment 8 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
89.35%
Method Description
A xenograft model derived from cell lines was established by unilateral subcutaneous injection of 1×10^6 HT-29 cells into female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, 99961.1-MMAE was administered at a dose of 10 mg/kg. The treatment was given twice a week for 4 weeks. The tumor inhibition rate was calculated at the end of the experiment.

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In Vivo Model HT-29-xenograft model
Experiment 9 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
91.74%
Method Description
A xenograft model derived from cell lines was established by injecting 1×10^7 Jeko-1 cells subcutaneously into the left side of female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, 99961.1-MMAE was administered at a dose of 10 mg/kg once. The tumor inhibition rate was calculated at the end of the experiment.
In Vivo Model Jeko-1-xenograft model
Experiment 10 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
95.77%
Method Description
A xenograft model derived from cell lines was established by injecting 1×10^7 Jeko cells subcutaneously into the left side of female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, 99961.1-MMAE was administered at a dose of 10 mg/kg. The treatment was given once a week for 3 weeks. The tumor inhibition rate was calculated at the end of the experiment.

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In Vivo Model Jeko-1-xenograft model
Experiment 11 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
96.60%
Method Description
A xenograft model derived from the cell line was established by injecting 1×10^6 MDA-MB-231 cells subcutaneously into the left side of female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, 99961.1-MMAE was administered at a dose of 10 mg/kg. The treatment was given once a week for 3 weeks. The tumor inhibition rate was calculated at the end of the experiment.

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In Vivo Model MDA-MB-231-xenograft model
Experiment 12 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
97.86%
Method Description
A xenograft model derived from the cell line was established by injecting 1×10^6 NCI-N87 cells subcutaneously into the left side of female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, 99961.1-MMAE was administered at a dose of 5 mg/kg. The treatment was given once a week for 3 weeks. The tumor inhibition rate was calculated at the end of the experiment.

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In Vivo Model NCI-N87-xenograft model
Experiment 13 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
98.21%
Method Description
A xenograft model derived from the cell line was established by injecting 1×10^7 MDA-MB-468 cells subcutaneously into the left side of female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, 99961.1-MMAE was administered at a dose of 5 mg/kg. The treatment was given once a week for 4 weeks. The tumor inhibition rate was calculated at the end of the experiment.

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In Vivo Model MDA-MB-468-xenograft model
Experiment 14 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
99.20%
Method Description
A xenograft model derived from the cell line was established by injecting 1×10^6 NCI-N87 cells subcutaneously into the left side of female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, 99961.1-MMAE was administered at a dose of 10 mg/kg. The treatment was given once a week for 3 weeks. The tumor inhibition rate was calculated at the end of the experiment.

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In Vivo Model NCI-N87-xenograft model
Experiment 15 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
100%
Method Description
A xenograft model derived from the cell line was established by injecting 1×10^7 MDA-MB-468 cells subcutaneously into the left side of female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, 99961.1-MMAE was administered at a dose of 10 mg/kg. The treatment was given once a week for 4 weeks. The tumor inhibition rate was calculated at the end of the experiment.

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In Vivo Model MDA-MB-468-xenograft model
References
Ref 1 Ror1-targeted binding molecules and their Applications