Payload Information

General Information of This Payload
Payload ID
PAY0UXSPW
Name
Lidamycin
Synonyms
C-1027; CHEBI:68320; lidamycin; CHEMBL506048; Q27136818; [(1R,7S,12R,13E,20R)-7-Amino-4-chloro-20-[(2S,3R,4R,5S)-5-(dimethylamino)-3,4-dihydroxy-6,6-dimethyloxan-2-yl]oxy-25-hydroxy-9-oxo-2,10-dioxatetracyclo[11.7.3.23,6.016,20]pentacosa-3(25),4,6(24),13(23),16,18-hexaen-14,21-diyn-12-yl] 7-methoxy-2-methylidene-3-oxo-4H-1,4-benzoxazine-5-carboxylate; 149438-20-0
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Target(s) Human Deoxyribonucleic acid (hDNA)
 Target Info 
Structure
Formula
C43H42ClN3O13
Isosmiles
CC1([C@H]([C@H]([C@H]([C@@H](O1)O[C@]23C=CC=C2C#C/C/4=C\C#C[C@H]3OC5=C(C=C(C=C5Cl)[C@H](CC(=O)OC[C@@H]4OC(=O)C6=C7C(=CC(=C6)OC)OC(=C)C(=O)N7)N)O)O)O)N(C)C)C
PubChem CID
9962646
InChI
InChI=1S/C43H42ClN3O13/c1-21-39(52)46-34-26(17-25(54-6)18-30(34)56-21)40(53)57-31-20-55-33(49)19-28(45)23-15-27(44)37(29(48)16-23)58-32-11-7-9-22(31)12-13-24-10-8-14-43(24,32)60-41-36(51)35(50)38(47(4)5)42(2,3)59-41/h8-10,14-18,28,31-32,35-36,38,41,48,50-51H,1,19-20,45H2,2-6H3,(H,46,52)/b22-9+/t28-,31-,32+,35-,36+,38-,41-,43+/m0/s1
InChIKey
DGGZCXUXASNDAC-QQNGCVSVSA-N
IUPAC Name
[(1R,7S,12R,13E,20R)-7-amino-4-chloro-20-[(2S,3R,4R,5S)-5-(dimethylamino)-3,4-dihydroxy-6,6-dimethyloxan-2-yl]oxy-25-hydroxy-9-oxo-2,10-dioxatetracyclo[11.7.3.23,6.016,20]pentacosa-3(25),4,6(24),13(23),16,18-hexaen-14,21-diyn-12-yl] 7-methoxy-2-methylidene-3-oxo-4H-1,4-benzoxazine-5-carboxylate
Pharmaceutical Properties
Molecule Weight
844.3
Polar area
218
Complexity
1970
xlogp Value
2
Heavy Count
60
Rot Bonds
7
Hbond acc
15
Hbond Donor
5
The activity data of This Payload
Standard Type Value Units Cell line Disease Model Cell line ID Reference
Half Maximal Inhibitory Concentration (IC50) 20 nM
P388 cells
Lymphoma
CVCL_7222 
[1]
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
Dualtargeting lidamycin ADC [Investigative]
 ADC Info 
Discovered Using Patient-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 56.63%±9.71% Positive EGFR expression (EGFR+++/++)
Method Description
PDX mice were administrated vehicle or DTLL at the LDMequivalent dose of 0.1 mg/kg once a week for 3 wk. Tumor volumes were measured after animals were sacrificed on Days 24 and 39, respectively. DTLL was administered via tail vein injection once a week for three weeks.
In Vivo Model Pancreatic cancer PDX model (PDX: PA1338)
Fv-LDP-D3-AE [Investigative]
 ADC Info 
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 64.00% (Day 28) High EGFR expression (EGFR+++)
Method Description
KYSE150 cells (5 10 6 cells/200 L) suspended in PBS were inoculated subcutaneously into the right armpit of athymic mice. When the tumor volume reached about 80mm3, nude mice were randomized into two groups (n=6, per group), a control group and a Fv-LDP-D3-AE (0.2 mg/kg) group. The drug treatment group was given by tail vein injection once a week for two consecutive weeks.

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In Vivo Model Esophageal squamous cell carcinoma CDX model
In Vitro Model Esophageal squamous cell carcinoma KYSE-150 cells CVCL_1348
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 73.00% (Day 28) High EGFR expression (EGFR+++)
Method Description
KYSE150 cells (5 10 6 cells/200 L) suspended in PBS were inoculated subcutaneously into the right armpit of athymic mice. When the tumor volume reached about 80mm3, nude mice were randomized into two groups (n=6, per group), a control group and a Fv-LDP-D3-AE (0.25 mg/kg) group. The drug treatment group was given by tail vein injection once a week for two consecutive weeks.

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In Vivo Model Esophageal squamous cell carcinoma CDX model
In Vitro Model Esophageal squamous cell carcinoma KYSE-150 cells CVCL_1348
Experiment 3 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 81.00% (Day 28) High EGFR expression (EGFR+++)
Method Description
KYSE150 cells (5 10 6 cells/200 L) suspended in PBS were inoculated subcutaneously into the right armpit of athymic mice. When the tumor volume reached about 80mm3, nude mice were randomized into two groups (n=6, per group), a control group and a Fv-LDP-D3-AE (0.5 mg/kg) group. The drug treatment group was given by tail vein injection once a week for two consecutive weeks.

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In Vivo Model Esophageal squamous cell carcinoma CDX model
In Vitro Model Esophageal squamous cell carcinoma KYSE-150 cells CVCL_1348
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)
33.00 ng/mL
High EGFR expression (EGFR+++)
Method Description
The CCK8 method was used to evaluate the cytotoxicity of Fv-LDP-D3 and Fv-LDP-D3-AE in KYSE150, KYSE520, and Eca109 cells.
In Vitro Model Esophageal squamous cell carcinoma KYSE-150 cells CVCL_1348
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
44.00 ng/mL
High EGFR expression (EGFR+++)
Method Description
The CCK8 method was used to evaluate the cytotoxicity of Fv-LDP-D3 and Fv-LDP-D3-AE in KYSE150, KYSE520, and Eca109 cells.
In Vitro Model Esophageal squamous cell carcinoma KYSE-520 cells CVCL_1355
Experiment 3 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
75.00 ng/mL
Moderate EGFR expression (EGFR++)
Method Description
The CCK8 method was used to evaluate the cytotoxicity of Fv-LDP-D3 and Fv-LDP-D3-AE in KYSE150, KYSE520, and Eca109 cells.
In Vitro Model Esophageal squamous cell carcinoma Eca-109 cells CVCL_6898
References
Ref 1 Evaluation of the potential cancer chemotherapeutic efficacy of natural product isolates employing in vivo hollow fiber tests. J Nat Prod. 2002 Jun;65(6):842-50. doi: 10.1021/np010322w.
Ref 2 Internal enhancement of DNA damage by a novel bispecific antibody-drug conjugate-like therapeutics via blockage of mTOR and PD-L1 signal pathways in pancreatic cancer. Cancer Med. 2019 Feb;8(2):643-655. doi: 10.1002/cam4.1974. Epub 2019 Jan 25.
Ref 3 A recombinant scFv antibody-based fusion protein that targets EGFR associated with IMPDH2 downregulation and its drug conjugate show therapeutic efficacy against esophageal cancer. Drug Deliv. 2022 Dec;29(1):1243-1256.

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