Payload Information

General Information of This Payload
Payload ID
PAY0KEIJX
Name
TAM470
Synonyms
TAM470; SCHEMBL16979627; HY-148128; CS-0612970
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Target(s) Microtubule (MT)
 Target Info 
Structure
Formula
C41H67N7O6S
Isosmiles
CCCN([C@H](C[C@H](C1=NC(=CS1)C(=O)N[C@@H](CC2=CC=C(C=C2)O)C[C@H](C)C(=O)NN)OCCC)C(C)C)C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H]3CCCCN3C
PubChem CID
118284090
InChI
InChI=1S/C41H67N7O6S/c1-9-19-48(41(53)36(27(6)11-3)45-39(52)33-14-12-13-20-47(33)8)34(26(4)5)24-35(54-21-10-2)40-44-32(25-55-40)38(51)43-30(22-28(7)37(50)46-42)23-29-15-17-31(49)18-16-29/h15-18,25-28,30,33-36,49H,9-14,19-24,42H2,1-8H3,(H,43,51)(H,45,52)(H,46,50)/t27-,28-,30+,33+,34+,35+,36-/m0/s1
InChIKey
WZNRAPVOSYSOAK-WPIAVMABSA-N
IUPAC Name
N-[(2R,4S)-5-hydrazinyl-1-(4-hydroxyphenyl)-4-methyl-5-oxopentan-2-yl]-2-[(1R,3R)-4-methyl-3-[[(2S,3S)-3-methyl-2-[[(2R)-1-methylpiperidine-2-carbonyl]amino]pentanoyl]-propylamino]-1-propoxypentyl]-1,3-thiazole-4-carboxamide
Pharmaceutical Properties
Molecule Weight
786.1
Polar area
208
Complexity
1190
xlogp Value
6.4
Heavy Count
55
Rot Bonds
22
Hbond acc
10
Hbond Donor
5
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
OMTX-705 [Phase 1]
 ADC Info 
Discovered Using Patient-derived Xenograft Model
Click To Hide/Show 14 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 29.40% (Day 50) High FAP expression (FAP+++)
Method Description
Activity of OMTX705 alone or combined with gemcitabine in the Panc 007 PDX model. Five-week-old Foxn1 nu/nu (nude) female mice were implanted subcutaneously with 23 mm 3 tumor pieces of Panc 007,a pancreatic cancer PDX model. OMTX705 was administered intraperitoneally (ip) 10 mg/kg once weekly.
In Vivo Model Pancreatic cancer PDX model (PDX: Panc 007)
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 34.50% (Day 30) Moderate FAP expression (FAP++)
Method Description
Activity of OMTX705 alone or combined with gemcitabine in the TNBC PDX model Breast 014. OMTX705 was given intravenously (iv) 10 mg/kg once weekly for four doses (q7dx4).
In Vivo Model Triple-negative breast cancer PDX model (PDX: Breast 014)
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 40.70% (Day 30) Moderate FAP expression (FAP++)
Method Description
Activity of OMTX705 alone or combined with gemcitabine in the TNBC PDX model Breast 014. OMTX705 in combination with PTX,OMTX705 intravenous (iv) 10 mg/kg once weekly for four doses (q7dx4). PTX intravenous (iv) 7.5 mg/kg once weekly for three doses (q7dx3) starting from week two.
In Vivo Model Triple-negative breast cancer PDX model (PDX: Breast 014)
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 49.30% (Day 37) Moderate FAP expression (FAP++)
Method Description
Activity of OMTX705 alone or combined with gemcitabine in the Lung 024 PDX model. Five-week-old Foxn1 nu/nu (nude) female mice were implanted subcutaneously with 23 mm 3 tumor pieces of Panc 007,a pancreatic cancer PDX model. OMTX705 was administered intraperitoneally (ip) at 10 mg/kg,twice in the first week.
In Vivo Model Lung cancer PDX model (PDX: Lung 024)
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 57.50% (Day 37) Moderate FAP expression (FAP++)
Method Description
Activity of OMTX705 alone or combined with gemcitabine in the Lung 024 PDX model. Lung adenocarcinoma Lung 024 PDX models treated with OMTX705 alone or combined with paclitaxel (PTX). OMTX705 and PTX were combined at a dose of 7.5 mg/kg of PTX administered intravenously once a week starting in the second week,and OMTX705 at a dose of 10 mg/kg administered by injection twice in the first week.

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In Vivo Model Lung cancer PDX model (PDX: Lung 024)
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 69.70% (Day 50) High FAP expression (FAP+++)
Method Description
Activity of OMTX705 alone or combined with gemcitabine in the Panc 007 PDX model. Five-week-old Foxn1 nu/nu (nude) female mice were implanted subcutaneously with 23 mm 3 tumor pieces of Panc 007,a pancreatic cancer PDX model. OMTX705 was administered intraperitoneally (ip) 20 mg/kg once weekly.
In Vivo Model Pancreatic cancer PDX model (PDX: Panc 007)
Experiment 7 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 71.60% (Day 37) Moderate FAP expression (FAP++)
Method Description
Activity of OMTX705 alone or combined with gemcitabine in the Lung 024 PDX model. Lung adenocarcinoma Lung 024 PDX models treated with OMTX705 alone or combined with paclitaxel (PTX). OMTX705 was administered intraperitoneally (ip) at 30 mg/kg,once per week.
In Vivo Model Lung cancer PDX model (PDX: Lung 024)
Experiment 8 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 74.00% (Day 33) High FAP expression (FAP+++)
Method Description
OMTX705 exhibits potent effect in immunodeficient PDX models of different solid tumors. Five-week-old Foxn1 nu/nu (nude) female mice were implanted subcutaneously with 23 mm 3 tumor pieces of Panc 007,a pancreatic cancer PDX model. OMTX705 was given intravenously (iv) 20 mg/kg once weekly for four doses (q7dx4).
In Vivo Model Pancreatic cancer PDX model (PDX: Panc 007)
Experiment 9 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 80.40% (Day 30) Moderate FAP expression (FAP++)
Method Description
Activity of OMTX705 alone or combined with gemcitabine in the TNBC PDX model Breast 014. OMTX705 was given intravenously (iv) 30 mg/kg once weekly for four doses (q7dx4).
In Vivo Model Triple-negative breast cancer PDX model (PDX: Breast 014)
Experiment 10 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 85.90% (Day 33) High FAP expression (FAP+++)
Method Description
OMTX705 exhibits potent effect in immunodeficient PDX models of different solid tumors. Five-week-old Foxn1 nu/nu (nude) female mice were implanted subcutaneously with 23 mm 3 tumor pieces of Panc 007,a pancreatic cancer PDX model. OMTX705 was given intravenously (iv) 30 mg/kg once weekly for four doses (q7dx4).
In Vivo Model Pancreatic cancer PDX model (PDX: Panc 007)
Experiment 11 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 85.90% (Day 33) High FAP expression (FAP+++)
Method Description
OMTX705 exhibits potent effect in immunodeficient PDX models of different solid tumors. Five-week-old Foxn1 nu/nu (nude) female mice were implanted subcutaneously with 23 mm 3 tumor pieces of Panc 007,a pancreatic cancer PDX model. OMTX705 was given intravenously (iv) 40 mg/kg once weekly for four doses (q7dx4).
In Vivo Model Pancreatic cancer PDX model (PDX: Panc 007)
Experiment 12 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 88.50% (Day 50) High FAP expression (FAP+++)
Method Description
Activity of OMTX705 alone or combined with gemcitabine in the Panc 007 PDX model. Five-week-old Foxn1 nu/nu (nude) female mice were implanted subcutaneously with 23 mm 3 tumor pieces of Panc 007,a pancreatic cancer PDX model. OMTX705 was administered intraperitoneally (ip) 10 mg/kg once weekly,whereas gemcitabine was administered intraperitoneally 50 mg/kgweekly starting in the second week.

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In Vivo Model Pancreatic cancer PDX model (PDX: Panc 007)
Experiment 13 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 91.10% (Day 33) High FAP expression (FAP+++)
Method Description
OMTX705 exhibits potent effect in immunodeficient PDX models of different solid tumors. Five-week-old Foxn1 nu/nu (nude) female mice were implanted subcutaneously with 23 mm 3 tumor pieces of Panc 007,a pancreatic cancer PDX model. OMTX705 was given intravenously (iv) 50 mg/kg once weekly for four doses (q7dx4).
In Vivo Model Pancreatic cancer PDX model (PDX: Panc 007)
Experiment 14 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 91.10% (Day 33) High FAP expression (FAP+++)
Method Description
OMTX705 exhibits potent effect in immunodeficient PDX models of different solid tumors. Five-week-old Foxn1 nu/nu (nude) female mice were implanted subcutaneously with 23 mm 3 tumor pieces of Panc 007,a pancreatic cancer PDX model. OMTX705 was given intravenously (iv) 60 mg/kg once weekly for four doses (q7dx4).
In Vivo Model Pancreatic cancer PDX model (PDX: Panc 007)
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 (IC50)
230.00 pM
High FAP expression (FAP+++)
Method Description
Cell viability in CAF07, HT1080-FAP, and HT1080-WT cells was analyzed via crystal violet staining after exposure to the indicated antibodies or free drug. Cells were treated for 120 hours with a serial dilution of antibodies (starting at 400 nmol/L) or free drugs (starting at 60 mol/L).
In Vitro Model Fibrosarcoma HT-1080 cells (FAP expression) CVCL_0317
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
400.00 nM
Moderate FAP expression (FAP++)
Method Description
Cell viability in CAF07, HT1080-FAP, and HT1080-WT cells was analyzed via crystal violet staining after exposure to the indicated antibodies or free drug. Cells were treated for 120 hours with a serial dilution of antibodies (starting at 400 nmol/L) or free drugs (starting at 60 mol/L).
In Vitro Model Normal CAF cells CVCL_R883
References
Ref 1 OMTX705, a Novel FAP-Targeting ADC Demonstrates Activity in Chemotherapy and Pembrolizumab-Resistant Solid Tumor Models. Clin Cancer Res. 2020 Jul 1;26(13):3420-3430.

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