Payload Information

General Information of This Payload

Payload ID	PAY0ENCSA
Name	Kinesin spindle protein (KSP) inhibitor 3f
Synonyms	KSP inhibitor 3f Click to Show/Hide
Target(s)	Kinesin-like protein KIF11 (KIF11)	Target Info

Each Antibody-drug Conjugate Related to This Payload

Full Information of The Activity Data of The ADC(s) Related to This Payload

Anti-B7H3 APDC 3f [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 Inhibition value (TGI)	≈ 90.04% (Day 30)	Positive B7H3 expression (B7H3 +++/++)
Method Description	Both APDCs (10 mg/kg) have been administered to B7H3-positive U251-glioma-tumor-bearing mice; 24hours after treatment, tumors and organs were collected.
In Vivo Model	U251 CDX model
In Vitro Model	Astrocytoma	U-251MG cells		CVCL_0021
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 50)	Positive B7H3 expression (B7H3 +++/++)
Method Description	In the B7H3-positive, slowly growing head and neck squamous cell carcinoma model SCC4, APDC 3 g at a dose of 10 mg/kg given 3 times in a weekly schedule which favorably compared to cisplatin and radiation therapy.
In Vivo Model	SCC4 CDX model
In Vitro Model	Tongue squamous cell carcinoma	SCC-4 cells		CVCL_1684

TWEAKR ADC 3f [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					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.30 nM	Positive TNFRSF12A expression (TNFRSF12A +++/++)
Method Description	Cytotoxicity of ADCs, SMOL KSP inhibitors, and payload metabolite were determined in TWEAKR-positive cancer cell lines 72 h after treatment with the Promega CellTiter Glo (CTG) cell viability assay according to manufacturers instructions.
In Vitro Model	Colon adenocarcinoma	LoVo cells		CVCL_0399
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.70 nM	Positive TNFRSF12A expression (TNFRSF12A +++/++)
Method Description	Cytotoxicity of ADCs, SMOL KSP inhibitors, and payload metabolite were determined in TWEAKR-positive cancer cell lines 72 h after treatment with the Promega CellTiter Glo (CTG) cell viability assay according to manufacturers instructions.
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.90 nM	Positive TNFRSF12A expression (TNFRSF12A +++/++)
Method Description	Cytotoxicity of ADCs, SMOL KSP inhibitors, and payload metabolite were determined in TWEAKR-positive cancer cell lines 72 h after treatment with the Promega CellTiter Glo (CTG) cell viability assay according to manufacturers instructions.
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186

References

Ref 1	Antibody-Prodrug Conjugates with KSP Inhibitors and Legumain-Mediated Metabolite Formation. Chemistry. 2019 Jun 21;25(35):8208-8213. doi: 10.1002/chem.201900441. Epub 2019 Apr 15.