General Information of This Payload
Payload ID
PAY0RINMR
Name
10NH2-11F-Camptothecin
Synonyms
10NH2-11F-Camptothecin
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Target DNA topoisomerase I (TOP1)
Structure
Formula
C20H16FN3O4
Isosmiles
CC[C@]1(O)C(C=C2C3=NC4=CC(F)=C(N)C=C4C=C3CN52)=C(COC1=O)C5=O
PubChem CID
166138669
InChI
InChI=1S/C20H16FN3O4/c1-2-20(27)12-5-16-17-10(3-9-4-14(22)13(21)6-15(9)23-17)7-24(16)18(25)11(12)8-28-19(20)26/h3-6,27H,2,7-8,22H2,1H3/t20-/m0/s1
InChIKey
DTFQCOHTHXUPMI-FQEVSTJZSA-N
Pharmaceutical Properties
Molecule Weight
381.363
Polar area
107.44
Complexity
1231.353615
xlogp Value
1.8009
Heavy Count
28
Rot Bonds
1
Hbond acc
7
Hbond Donor
2
The activity data of This Payload
Standard Type Value Units Cell line Disease Model Cell line ID Reference
Half maximal inhibitory Concentration (lC50) 0.26 nM
SK-BR-3 cells
Breast adenocarcinoma
CVCL_0033 
[1]
Half maximal inhibitory Concentration (lC50) 0.26 nM
SK-BR-3 cells
Breast adenocarcinoma
CVCL_0033 
[1]
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
38354417 T-DL9 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.51 nM
High HER2 expression (HER2 +++)
Method Description
A total of 30,000 SK-BR-3 (HER2-high) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 30 nM Negative HER2 expression (HER2-)
Method Description
A total of 10,000 MDA-MB-468 (HER2-negative) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
References
Ref 1 Design and Evaluation of ZD06519, a Novel Camptothecin Payload for Antibody Drug Conjugates