Payload Information

General Information of This Payload
Payload ID
PAY0JYSRJ
Name
Auristatin M
Synonyms
Auristatin M
   Click to Show/Hide
Target(s) Microtubule (MT)
 Target Info 
Structure
Formula
C36H67N5O8S
Isosmiles
CCC(C)C(C(CC(=O)N1CCCC1C(OC)C(C)C(=O)NC(CCSC)C(=O)O)OC)N(C)C(=O)C(NC(=O)C(C(C)C)N(C)C)C(C)C
InChI
InChI=1S/C36H67N5O8S/c1-14-23(6)31(40(10)35(45)29(21(2)3)38-34(44)30(22(4)5)39(8)9)27(48-11)20-28(42)41-18-15-16-26(41)32(49-12)24(7)33(43)37-25(36(46)47)17-19-50-13/h21-27,29-32H,14-20H2,1-13H3,(H,37,43)(H,38,44)(H,46,47)
InChIKey
STYIZAGDTRHYON-UHFFFAOYSA-N
Pharmaceutical Properties
Molecule Weight
730.026
Polar area
157.82
Complexity
50
xlogp Value
2.9562
Heavy Count
50
Rot Bonds
22
Hbond acc
9
Hbond Donor
3
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
1F6-Asn- (D)Lys-AM [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 [1]
Efficacy Data Tumor Growth Inhibition value (TGI)
93.91% (Day 30)
Positive TNF expression (TNF+++/++)
Method Description
1 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 [1]
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 2 Reporting the Activity Date of This ADC [1]
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 Clear cell renal cell carcinoma Caki-1 cells CVCL_0234
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
28.00 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-AM [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)
39.00 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 [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
56.00 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 [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1000.00 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
References
Ref 1 Novel Peptide Linkers for Highly Potent Antibody-Auristatin Conjugate.

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