Linker Information

General Information of This Linker

Linker ID	LIN0IAVKF
Linker Name	Mal-PEG4-DBCO-Ala-Val
Linker Type	Cathepsin-cleavable linker
Antibody-Linker Relation	Cleavable
Structure
Structure	3D MOL		2D MOL
Formula	C48H65N9O12
Isosmiles	CC(NC(=O)C(C(C)C)N(C)CCCn1nnc2c1-c1ccccc1CN(C(=O)CCNC(=O)CCOCCOCCOCCOCCNC(=O)CCN1C(=O)C=CC1=O)c1ccccc1-2)C(=O)O
InChI	InChI=1S/C48H65N9O12/c1-33(2)45(47(63)51-34(3)48(64)65)54(4)21-9-22-57-46-36-11-6-5-10-35(36)32-56(38-13-8-7-12-37(38)44(46)52-53-57)43(62)16-19-49-40(59)18-24-66-26-28-68-30-31-69-29-27-67-25-20-50-39(58)17-23-55-41(60)14-15-42(55)61/h5-8,10-15,33-34,45H,9,16-32H2,1-4H3,(H,49,59)(H,50,58)(H,51,63)(H,64,65)
InChIKey	ICAMVROXGLTTRY-UHFFFAOYSA-N
Pharmaceutical Properties	Molecule Weight	960.099	Polar area	253.16
	Complexity	69	xlogp Value	1.7886
	Heavy Count	69	Rot Bonds	30
	Hbond acc	15	Hbond Donor	4

Each Antibody-drug Conjugate Related to This Linker

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

Milatuzumab-RSL3-NH2 [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					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.40 nM	High CD74 expression (CD74+++)
Method Description	The inhibitory activity of Milatuzumab-RSL3-NH2 against cancer cell growth was evaluated by MTT cytotoxicity assay.
In Vitro Model	Diffuse large B-cell lymphoma	Toledo cells		CVCL_3611

Trastuzumab-RSL3-NH2 [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					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	100.00 nM	High HER2 expression (HER2+++)
Method Description	The inhibitory activity of Trastuzumab-RSL3-NH2 against cancer cell growth was evaluated by MTT cytotoxicity assay.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

References

Ref 1	The first ADC bearing the ferroptosis inducer RSL3 as a payload with conservation of the fragile electrophilic warhead. Eur J Med Chem. 2022 Dec 15;244:114863.