Payload Information
General Information of This Payload
| Payload ID | PAY0UMYYX |
|||||
|---|---|---|---|---|---|---|
| Name | Compound 5 |
|||||
| Synonyms |
compound 5
Click to Show/Hide
|
|||||
| Target | DNA topoisomerase I (TOP1) | |||||
| Structure |
|
|||||
| Formula | C27H23F4N3O6 |
|||||
| Isosmiles | CC1=C(C2=C3C=C1F)CC[C@H](NC([C@@H](C(F)(F)F)O)=O)C2=C(C(C4=CC([C@@]5(O)CC)=C6COC5=O)=N3)CN4C6=O |
|||||
| InChI |
InChI=1S/C27H23F4N3O6/c1-3-26(39)14-6-18-21-12(8-34(18)24(37)13(14)9-40-25(26)38)20-16(33-23(36)22(35)27(29,30)31)5-4-11-10(2)15(28)7-17(32-21)19(11)20/h6-7,16,22,35,39H,3-5,8-9H2,1-2H3,(H,33,36)/t16-,22-,26-/m0/s1
|
|||||
| InChIKey |
PVDTZIJCQHIVRL-YZKRRQQXSA-N
|
|||||
| Pharmaceutical Properties | Molecule Weight |
561.488 |
Polar area |
130.75 |
||
Complexity |
1659.559866 |
xlogp Value |
2.55382 |
|||
Heavy Count |
40 |
Rot Bonds |
3 |
|||
Hbond acc |
8 |
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
cN113943310A ADC-15 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) |
95.96%
|
Positive HER2 expression (HER2+++/++) | ||
| Method Description |
3x104 A431 cells were injected subcutaneously into the right shoulder of 4-6-week-old BALB/c nude mice, and when the average tumor size of the mice grew to 140 ~ 150mm3, they were randomly divided into 5 cells in each group. At day 0, day 7, day 14, day 21, intravenous injection of a blank control (blank buffer solution) and a dose of 10mg/kg antibody drug conjugate was administered. The tumor volume was measured at day 0, day 7, day 14, day 21, day 24, day 28, day 32, day 36 and the tumor growth inhibition rate on day 28 of d was calculated.
Click to Show/Hide
|
||||
| In Vivo Model | A431 tumor bearing nude mouse model | ||||
isumab04-C5 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.26 pM
|
High FRa expression (FRa +++) | ||
| Method Description |
A Cell line test on Colo205
|
||||
| In Vitro Model | Colon adenocarcinoma | Colo205 cells | CVCL_0218 | ||
isumab01-C5 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
4 pM
|
High FRa expression (FRa +++) | ||
| Method Description |
A Cell line test on Jeg3
|
||||
| In Vitro Model | Gestational choriocarcinoma | Jeg3 cells | CVCL_0363 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
28 pM
|
High FRa expression (FRa +++) | ||
| Method Description |
A Cell line test on H2110
|
||||
| In Vitro Model | Lung non-small cell carcinoma | H2110 cells | CVCL_1530 | ||
References