Payload Information

General Information of This Payload
Payload ID
PAY0KGVAS
Name
Auristatin F
Synonyms
Auristatin F; 163768-50-1; ((2R,3R)-3-((S)-1-((3R,4S,5S)-4-((S)-2-((S)-2-(dimethylamino)-3-methylbutanamido)-N,3-dimethylbutanamido)-3-methoxy-5-methylheptanoyl)pyrrolidin-2-yl)-3-methoxy-2-methylpropanoyl)-L-phenylalanine; (2S)-2-[[(2R,3R)-3-[(2S)-1-[(3R,4S,5S)-4-[[(2S)-2-[[(2S)-2-(dimethylamino)-3-methylbutanoyl]amino]-3-methylbutanoyl]-methylamino]-3-methoxy-5-methylheptanoyl]pyrrolidin-2-yl]-3-methoxy-2-methylpropanoyl]amino]-3-phenylpropanoic acid; SCHEMBL2606135; CHEMBL5184029; LGNCNVVZCUVPOT-FUVGGWJZSA-N; EX-A3361; CS-3436; BP-27999; HY-15583; F85072; (2S)-2-[(2R)-2-[(R)-[(2S)-1-[(3R,4S,5S)-4-[(2S)-2-[(2S)-2-(dimethylamino)-3-methylbutanamido]-N,3-dimethylbutanamido]-3-methoxy-5-methylheptanoyl]pyrrolidin-2-yl](methoxy)methyl]propanamido]-3-phenylpropanoic acid; (S)-2-((2R,3R)-3-((S)-1-((3R,4S,5S)-4-((S)-2-((S)-2-(Dimethylamino)-3-methylbutanamido)-N,3-dimethylbutanamido)-3-methoxy-5-methylheptanoyl)pyrrolidin-2-yl)-3-methoxy-2-methylpropanamido)-3-phenylpropanoic acid
   Click to Show/Hide
Target(s) Microtubule (MT)
 Target Info 
Structure
Formula
C40H67N5O8
Isosmiles
CC[C@H](C)[C@@H]([C@@H](CC(=O)N1CCC[C@H]1[C@@H]([C@@H](C)C(=O)N[C@@H](CC2=CC=CC=C2)C(=O)O)OC)OC)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@H](C(C)C)N(C)C
PubChem CID
67472795
InChI
InChI=1S/C40H67N5O8/c1-13-26(6)35(44(10)39(49)33(24(2)3)42-38(48)34(25(4)5)43(8)9)31(52-11)23-32(46)45-21-17-20-30(45)36(53-12)27(7)37(47)41-29(40(50)51)22-28-18-15-14-16-19-28/h14-16,18-19,24-27,29-31,33-36H,13,17,20-23H2,1-12H3,(H,41,47)(H,42,48)(H,50,51)/t26-,27+,29-,30-,31+,33-,34-,35-,36+/m0/s1
InChIKey
LGNCNVVZCUVPOT-FUVGGWJZSA-N
IUPAC Name
(2S)-2-[[(2R,3R)-3-[(2S)-1-[(3R,4S,5S)-4-[[(2S)-2-[[(2S)-2-(dimethylamino)-3-methylbutanoyl]amino]-3-methylbutanoyl]-methylamino]-3-methoxy-5-methylheptanoyl]pyrrolidin-2-yl]-3-methoxy-2-methylpropanoyl]amino]-3-phenylpropanoic acid
Pharmaceutical Properties
Molecule Weight
746
Polar area
158
Complexity
1190
xlogp Value
2.6
Heavy Count
53
Rot Bonds
21
Hbond acc
9
Hbond Donor
3
The activity data of This Payload
Standard Type Value Units Cell line Disease Model Cell line ID Reference
Half Maximal Inhibitory Concentration (IC50) 105 nM
Panel NCI-60 cells
Normal
Undisclosed [1]
Half Maximal Inhibitory Concentration (IC50) 37.7 nM
NCI-H1299 cells (MMAE resistant)
Lung large cell carcinoma
CVCL_0060 
[2]
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
1F6-beta-Ala- (D)Asp-AF [Investigative]
 ADC Info 
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI)
19.75% (Day 30)
Positive TNF expression (TNF+++/++)
Method Description
3 mg mAb component/kg in vivo therapeutic efficacy of the conjugates in nude mice(5 animals/group).
In Vivo Model 786-O human RCC cell line xenograft model
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
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 [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
525.00 ng/mL
Positive CD70 expression (CD70+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1096.00 ng/mL
Positive CD70 expression (CD70+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Hodgkin lymphoma L-428 cells CVCL_1361
Experiment 3 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1585.00 ng/mL
Positive CD70 expression (CD70+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Clear cell renal cell carcinoma Caki-1 cells CVCL_0234
1F6-Me3-Lys-Pro-AF [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 [3]
Efficacy Data Tumor Growth Inhibition value (TGI)
66.35% (Day 30)
Positive TNF expression (TNF+++/++)
Method Description
3 mg mAb component/kg in vivo therapeutic efficacy of the conjugates in nude mice(5 animals/group).
In Vivo Model DBTRG-05MG glioblastoma cell line xenograft model
In Vitro Model Anaplastic astrocytoma DBTRG-05MG cells CVCL_1169
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI)
93.15% (Day 30)
Positive TNF expression (TNF+++/++)
Method Description
3 mg mAb component/kg in vivo therapeutic efficacy of the conjugates in nude mice(5 animals/group).
In Vivo Model 786-O human RCC cell line xenograft model
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
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 [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
11.00 ng/mL
Positive TNF expression (TNF+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Clear cell renal cell carcinoma Caki-1 cells CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
20.00 ng/mL
Positive TNF expression (TNF+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
Experiment 3 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
24.00 ng/mL
Positive TNF expression (TNF+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Hodgkin lymphoma L-428 cells CVCL_1361
1F6-Met- (D)Lys-AF [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 [3]
Efficacy Data Tumor Growth Inhibition value (TGI)
86.68% (Day 30)
Positive TNF expression (TNF+++/++)
Method Description
3 mg mAb component/kg in vivo therapeutic efficacy of the conjugates in nude mice(5 animals/group).
In Vivo Model DBTRG-05MG glioblastoma cell line xenograft model
In Vitro Model Anaplastic astrocytoma DBTRG-05MG cells CVCL_1169
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI)
92.40% (Day 30)
Positive TNF expression (TNF+++/++)
Method Description
3 mg mAb component/kg in vivo therapeutic efficacy of the conjugates in nude mice(5 animals/group).
In Vivo Model 786-O human RCC cell line xenograft model
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
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 [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
9.00 ng/mL
Positive TNF expression (TNF+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Clear cell renal cell carcinoma Caki-1 cells CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
12.00 ng/mL
Positive TNF expression (TNF+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
Experiment 3 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
168.00 ng/mL
Positive TNF expression (TNF+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Hodgkin lymphoma L-428 cells CVCL_1361
1F6-NorVal- (D)Asp-AF [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 [3]
Efficacy Data Tumor Growth Inhibition value (TGI)
92.33% (Day 30)
Positive TNF expression (TNF+++/++)
Method Description
3 mg mAb component/kg in vivo therapeutic efficacy of the conjugates in nude mice(5 animals/group).
In Vivo Model DBTRG-05MG glioblastoma cell line xenograft model
In Vitro Model Anaplastic astrocytoma DBTRG-05MG cells CVCL_1169
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI)
95.90% (Day 30)
Positive TNF expression (TNF+++/++)
Method Description
3 mg mAb component/kg in vivo therapeutic efficacy of the conjugates in nude mice(5 animals/group).
In Vivo Model 786-O human RCC cell line xenograft model
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
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 [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
12.00 ng/mL
Positive CD70 expression (CD70+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Clear cell renal cell carcinoma Caki-1 cells CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
24.00 ng/mL
Positive CD70 expression (CD70+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Hodgkin lymphoma L-428 cells CVCL_1361
Experiment 3 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
28.00 ng/mL
Positive CD70 expression (CD70+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
1F6-PhenylGly- (D)Lys-AF [Investigative]
 ADC Info 
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI)
93.39% (Day 30)
Positive TNF expression (TNF+++/++)
Method Description
3 mg mAb component/kg in vivo therapeutic efficacy of the conjugates in nude mice(5 animals/group).
In Vivo Model 786-O human RCC cell line xenograft model
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
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 [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
44.00 ng/mL
Positive TNF expression (TNF+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Clear cell renal cell carcinoma Caki-1 cells CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
275.00 ng/mL
Positive TNF expression (TNF+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Hodgkin lymphoma L-428 cells CVCL_1361
Experiment 3 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
339.00 ng/mL
Positive TNF expression (TNF+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
1F6-Ile-Pro-AF [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 [3]
Efficacy Data Tumor Growth Inhibition value (TGI)
95.00% (Day 30)
Positive TNF expression (TNF+++/++)
Method Description
3 mg mAb component/kg in vivo therapeutic efficacy of the conjugates in nude mice(5 animals/group).
In Vivo Model DBTRG-05MG glioblastoma cell line xenograft model
In Vitro Model Anaplastic astrocytoma DBTRG-05MG cells CVCL_1169
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI)
98.65% (Day 30)
Positive TNF expression (TNF+++/++)
Method Description
3 mg mAb component/kg in vivo therapeutic efficacy of the conjugates in nude mice(5 animals/group).
In Vivo Model 786-O human RCC cell line xenograft model
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
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 [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
5.00 ng/mL
Positive TNF expression (TNF+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Hodgkin lymphoma L-428 cells CVCL_1361
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
9.00 ng/mL
Positive TNF expression (TNF+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Clear cell renal cell carcinoma Caki-1 cells CVCL_0234
Experiment 3 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
10.00 ng/mL
Positive TNF expression (TNF+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
1F6-Met-Lys-AF [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 [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
3.00 ng/mL
Positive CD70 expression (CD70+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Hodgkin lymphoma L-428 cells CVCL_1361
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
4.00 ng/mL
Positive CD70 expression (CD70+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Clear cell renal cell carcinoma Caki-1 cells CVCL_0234
Experiment 3 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
7.00 ng/mL
Positive CD70 expression (CD70+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
1F6-Ile-Val-AF [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 [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
3.00 ng/mL
Positive CD70 expression (CD70+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
3.00 ng/mL
Positive CD70 expression (CD70+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Hodgkin lymphoma L-428 cells CVCL_1361
Experiment 3 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
4.00 ng/mL
Positive CD70 expression (CD70+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Clear cell renal cell carcinoma Caki-1 cells CVCL_0234
1F6-His-Val-AF [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 [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
6.00 ng/mL
Positive CD70 expression (CD70+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
6.00 ng/mL
Positive CD70 expression (CD70+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Hodgkin lymphoma L-428 cells CVCL_1361
Experiment 3 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
11.00 ng/mL
Positive CD70 expression (CD70+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Clear cell renal cell carcinoma Caki-1 cells CVCL_0234
1F6-Asp-Val-AF [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 6 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
8.00 ng/mL
Positive CD70 expression (CD70+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Clear cell renal cell carcinoma Caki-1 cells CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
8.00 ng/mL
Positive CD70 expression (CD70+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Hodgkin lymphoma L-428 cells CVCL_1361
Experiment 3 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
9.00 ng/mL
Positive CD70 expression (CD70+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
Experiment 4 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
18.00 ng/mL
Positive CD70 expression (CD70+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
Experiment 5 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
18.00 ng/mL
Positive CD70 expression (CD70+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Hodgkin lymphoma L-428 cells CVCL_1361
Experiment 6 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
25.00 ng/mL
Positive CD70 expression (CD70+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Clear cell renal cell carcinoma Caki-1 cells CVCL_0234
1711 (scFv)-SNAP-AuriF [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 [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.52 uM
High EGFR expression (EGFR+++)
Method Description
XTT viability assay was used to assess cytotoxicity following a 72 h incubation with 1711 (scFv)-SNAP-AuriF on MDA-MB-468.
In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
1F6-Pro- (D)Lys-AF [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 [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10.00 uM Positive TNF expression (TNF+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10.00 uM Positive TNF expression (TNF+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Clear cell renal cell carcinoma Caki-1 cells CVCL_0234
Experiment 3 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10.00 uM Positive TNF expression (TNF+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Hodgkin lymphoma L-428 cells CVCL_1361
References
Ref 1 Discovery and Development of Dolastatin 10-Derived Antibody Drug Conjugate Anticancer Drugs. J Nat Prod. 2022 Mar 25;85(3):666-687. doi: 10.1021/acs.jnatprod.1c01135. Epub 2022 Jan 24.
Ref 2 Synthesis and biological activity of analogues of the antimicrotubule agent N,beta,beta-trimethyl-L-phenylalanyl-N(1)-[(1S,2E)-3-carboxy-1-isopropylbut-2-enyl]- N(1),3-dimethyl-L-valinamide (HTI-286). J Med Chem. 2004 Sep 9;47(19):4774-86. doi: 10.1021/jm040056u.
Ref 3 Novel Peptide Linkers for Highly Potent Antibody-Auristatin Conjugate.
Ref 4 Click Chemistry-Generated Auristatin F-Linker-Benzylguanine for a SNAP-Tag-Based Recombinant Antibody-Drug Conjugate Demonstrating Selective Cytotoxicity toward EGFR-Overexpressing Tumor Cells. ACS Omega. 2023 Jan 17;8(4):4026-4037. doi: 10.1021/acsomega.2c06844. eCollection 2023 Jan 31.

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