Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0JFLNE
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| ADC Name |
CO20240013452A2 99961-MMAE
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| Synonyms |
CO20240013452A2 99961-MMAE
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| Organization |
HANGZHOU ZHONGMEIHUADONG PHARMACEUTICAL CO. LTD. | SANYOU BIOPHARMACEUTICALS CO. LTD.
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| Drug Status |
Investigative
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| Antibody Name |
99961.1
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Antibody Info | ||||
| Antigen Name |
Inactive tyrosine-protein kinase transmembrane receptor ROR1 (ROR1)
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Antigen Info | ||||
| Payload Name |
Monomethyl auristatin E
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Payload Info | ||||
| Therapeutic Target |
Microtubule (MT)
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Target Info | ||||
| Linker Name |
Mc-Val-Cit-PABC
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Linker Info | ||||
General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Revealed Based on the Cell Line Data
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) | 11.08% | Positive ROR1 expression (ROR1+++/++) | ||
| Method Description |
Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously withHT-29 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (0.4 mg/kg) (BIWƨ).
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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% | Positive ROR1 expression (ROR1+++/++) | ||
| Method Description |
Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously withHT-29 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (2 mg/kg) (BIWƨ).
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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% | Positive ROR1 expression (ROR1+++/++) | ||
| Method Description |
Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously with Jeko-1 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (2.5 mg/kg- D15, 3.5 mg/kg- D29) (Q2WƦ).
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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% | Positive ROR1 expression (ROR1+++/++) | ||
| Method Description |
Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously with A549 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (10 mg/kg) (BIWƧ).
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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% | Positive ROR1 expression (ROR1+++/++) | ||
| Method Description |
Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously with Jeko-1 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (2.5 mg/kg) (QWƧ).
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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% | Positive ROR1 expression (ROR1+++/++) | ||
| Method Description |
Female NOD SCID nude mice between 6-8 weeks of age were injected subcutaneously with MDA-MB-4681 cells, when tumors reached appproximately 200 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (10 mg/kg) once.
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| 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% | Positive ROR1 expression (ROR1+++/++) | ||
| Method Description |
Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously with MDA-MB-231 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (5 mg/kg) (QWƧ).
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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% | Positive ROR1 expression (ROR1+++/++) | ||
| Method Description |
Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously withHT-29 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (10 mg/kg) (BIWƨ).
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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% | Positive ROR1 expression (ROR1+++/++) | ||
| Method Description |
Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously with Jeko-1 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (10 mg/kg) once.
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| 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% | Positive ROR1 expression (ROR1+++/++) | ||
| Method Description |
Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously with Jeko-1 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (10 mg/kg) (QWƧ).
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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% | Positive ROR1 expression (ROR1+++/++) | ||
| Method Description |
Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously with MDA-MB-231 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (10 mg/kg) (QWƧ).
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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% | Positive ROR1 expression (ROR1+++/++) | ||
| Method Description |
Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously with NCI-N87 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (5 mg/kg) (QWƧ).
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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% | Positive ROR1 expression (ROR1+++/++) | ||
| Method Description |
Female NOD SCID nude mice between 6-8 weeks of age were injected subcutaneously with MDA-MB-4681 cells, when tumors reached appproximately 200 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (5 mg/kg) (QWƧ).
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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% | Positive ROR1 expression (ROR1+++/++) | ||
| Method Description |
Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously with NCI-N87 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (10 mg/kg) (QWƧ).
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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% | Positive ROR1 expression (ROR1+++/++) | ||
| Method Description |
Female NOD SCID nude mice between 6-8 weeks of age were injected subcutaneously with MDA-MB-4681 cells, when tumors reached appproximately 200 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (10 mg/kg) (QWƧ).
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| In Vivo Model | MDA-MB-468 xenograft model | ||||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
21.22 nM
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| Method Description |
ADCs were tested in MDA-MB-468 cells, and were added at final working concentration at 500 nM, 158 nM, 50 nM, 15.8 nM, 5 nM, 1.58 nM, 0.5 nM, 0.158 nM, 0.05 Nm, incubated for 3 days.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
44.56 nM
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| Method Description |
ADCs were tested in Jeko-1 cells, and were added at final working concentration at 500 nM, 158 nM, 50 nM, 15.8 nM, 5 nM, 1.58 nM, 0.5 nM, 0.158 nM, 0.05 Nm, incubated for 3 days.
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| In Vitro Model | Mantle cell lymphoma | JeKo-1 cells | CVCL_1865 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
82.09 nM
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| Method Description |
ADCs were tested in HT-29 cells, and were added at final working concentration at 2000 nM, 500 nM, 250 nM, 125 nM, 62.5 nM, 31.25 nM, 15.625 nM, 7.813 nM, 1.953 nM, incubated for 4 days.
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| In Vitro Model | Colon adenocarcinoma | HT-29 cells | CVCL_0320 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
102.8 nM
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| Method Description |
ADCs were tested in NCI-H1944 cells, and were added at final working concentration at 500 nM, 158 nM, 50 nM, 15.8 nM, 5 nM, 1.58 nM, 0.5 nM, 0.158 nM, 0.05 Nm, incubated for 3 days.
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| In Vitro Model | Lung adenocarcinoma | NCI-H1944 cells | CVCL_1508 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
295.6 nM
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| Method Description |
ADCs were tested in A549 cells, and were added at final working concentration at 2000 nM, 500 nM, 250 nM, 125 nM, 62.5 nM, 31.25 nM, 15.625 nM, 7.813 nM, 1.953 nM, incubated for 3 days.
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| In Vitro Model | Lung adenocarcinoma | A549 cells | CVCL_0023 | ||