Linker Information

General Information of This Linker
Linker ID
LIN0EAPPJ
Linker Name
DMBA-SIL
Linker Type
X-ray responsive linker
Antibody-Linker Relation
Cleavable
Structure
Formula
C26H24N2O11
Isosmiles
COC(=O)C(OC(=O)Oc1ccc([N+](=O)[O-])cc1)c1ccc(NC(=O)OCc2cc(OC)cc(OC)c2)cc1
InChI
InChI=1S/C26H24N2O11/c1-34-21-12-16(13-22(14-21)35-2)15-37-25(30)27-18-6-4-17(5-7-18)23(24(29)36-3)39-26(31)38-20-10-8-19(9-11-20)28(32)33/h4-14,23H,15H2,1-3H3,(H,27,30)
InChIKey
ZZRDZSLWFXWULS-UHFFFAOYSA-N
Pharmaceutical Properties
Molecule Weight
540.481
Polar area
161.76
Complexity
39
xlogp Value
4.7904
Heavy Count
39
Rot Bonds
10
Hbond acc
11
Hbond Donor
1
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
MAb-DMBA-SIL-MMAE [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)
0.10 nM
Method Description
Cytotoxicity of non-irradiated or X-ray-irradiated (8 Gy) mAb-DMBA-SIL-MMAE conjugate in comparison to free MMAE in anaplastic thyroid cancer.
In Vitro Model Thyroid gland anaplastic carcinoma 8505C cells CVCL_1054
Alb-DMBA-SIL-MMAE [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.76 nM
Method Description
The inhibitory activity of Alb-DMBA-SIL-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro. Caged and conjugated MMAE is selectively cytotoxic and activated by X-ray irradiation.
In Vitro Model Thyroid gland anaplastic carcinoma 8505C cells CVCL_1054
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
2.00 nM
Method Description
The inhibitory activity of Alb-DMBA-SIL-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro. Caged and conjugated MMAE is selectively cytotoxic and activated by X-ray irradiation.
In Vitro Model Mouse colon adenocarcinoma MC-38 cells CVCL_B288
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
7.29 nM
Low FOLR1 expression (FOLR1+)
Method Description
The inhibitory activity of Alb-DMBA-SIL-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro. Caged and conjugated MMAE is selectively cytotoxic and activated by X-ray irradiation.
In Vitro Model Acute erythroid leukemia TBP-3743 cancer cells Mus musculus
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
8.92 nM
Method Description
The inhibitory activity of Alb-DMBA-SIL-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro. Caged and conjugated MMAE is selectively cytotoxic and activated by X-ray irradiation.
In Vitro Model Oral cavity squamous cell carcinoma MOC-L2 cells CVCL_A9X4
Experiment 5 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Effective Concentration (EC50)
1.40 nM
Method Description
The inhibitory activity of Alb-DMBA-SIL-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro. Caged and conjugated MMAE is selectively cytotoxic and activated by X-ray irradiation.
In Vitro Model Skin squamous cell carcinoma A431 cells CVCL_0037
Alb-DMBA-SIL-DOX [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 (IC50)
21.41 nM
Method Description
The inhibitory activity of Alb-DMBA-SIL-DOX against cancer cell growth was evaluated in various human cancer cell lines in vitro. Caged and conjugated DOX is selectively cytotoxic and activated by X-ray irradiation.
In Vitro Model Acute erythroid leukemia TBP-3743 cancer cells Mus musculus
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
35.57 nM
Method Description
The inhibitory activity of Alb-DMBA-SIL-DOX against cancer cell growth was evaluated in various human cancer cell lines in vitro. Caged and conjugated DOX is selectively cytotoxic and activated by X-ray irradiation.
In Vitro Model Thyroid gland anaplastic carcinoma 8505C cells CVCL_1054
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
52.13 nM
Method Description
The inhibitory activity of Alb-DMBA-SIL-DOX against cancer cell growth was evaluated in various human cancer cell lines in vitro. Caged and conjugated DOX is selectively cytotoxic and activated by X-ray irradiation.
In Vitro Model Mouse colon adenocarcinoma MC-38 cells CVCL_B288
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
224.40 nM
Method Description
The inhibitory activity of Alb-DMBA-SIL-DOX against cancer cell growth was evaluated in various human cancer cell lines in vitro. Caged and conjugated DOX is selectively cytotoxic and activated by X-ray irradiation.
In Vitro Model Oral cavity squamous cell carcinoma MOC-L2 cells CVCL_A9X4
References
Ref 1 Radiation Cleaved Drug-Conjugate Linkers Enable Local Payload Release. Bioconjug Chem. 2022 Aug 17;33(8):1474-1484.
Ref 2 Discovery of STRO-002, a Novel Homogeneous ADC Targeting Folate Receptor Alpha, for the Treatment of Ovarian and Endometrial Cancers. Mol Cancer Ther. 2023 Feb 1;22(2):155-167.

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