General Information of This Payload
Payload ID
PAY0JODQA
Name
CN119343152A Trastuzumab-Example6 Payload
Synonyms
CN119343152A Trastuzumab-Example6 Payload
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Target DNA topoisomerase I (TOP1)
Structure
Formula
C25H22FN3O6
Isosmiles
CC[C@@](C(C=C1C2=NC3=CC(F)=C(C)C4=C3C([C@@H](NC(O)=O)CC4)=C2CN51)=C(C5=O)CO6)(O)C6=O
InChI
InChI=1S/C25H22FN3O6/c1-3-25(34)14-6-18-21-12(8-29(18)22(30)13(14)9-35-23(25)31)20-16(28-24(32)33)5-4-11-10(2)15(26)7-17(27-21)19(11)20/h6-7,16,28,34H,3-5,8-9H2,1-2H3,(H,32,33)/t16-,25-/m0/s1
InChIKey
QYYIJXHUUIMSES-LMKMVOKYSA-N
Pharmaceutical Properties
Molecule Weight
479.464
Polar area
130.75
Complexity
1518.594434
xlogp Value
2.78202
Heavy Count
35
Rot Bonds
2
Hbond acc
7
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
Trastuzumab-Example 6 [Investigative]
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 (lC50)
0.0208 nM
High HER2 expression (HER2 +++)
Method Description
On the day of administration, HER2 targeted ADC and HER2 were prepared at a 10 fold ratio in standard growth medium. Add the prepared targeted ADC treatment to cells to obtain a final concentration of 3.81e-5nM to 100nM and a final volume of 50uL/well. Each drug concentration is tested in quadruplicate. On the same day, the cell viability of untreated cells at the time of administration was evaluated by adding 25 u L of CellTiter (ProMag catalog number G7573), a reagent for lysing cells and measuring total adenosine triphosphate (ATP) content. Incubate the plate at room temperature for 10 minutes to stabilize the luminescence signal before reading. Use luminous readingThe PHERAstar FSX ELISA reader (BMG Labtech) was used to measure the luminescence signals of all plates. This signal represents the cell viability of untreated cells on the day of administration or day 0.

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In Vitro Model Invasive breast carcinoma BT-474 cells CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.076 nM
High HER2 expression (HER2 +++)
Method Description
On the day of administration, HER2 targeted ADC and HER2 were prepared at a 10 fold ratio in standard growth medium. Add the prepared targeted ADC treatment to cells to obtain a final concentration of 3.81e-5nM to 100nM and a final volume of 50uL/well. Each drug concentration is tested in quadruplicate. On the same day, the cell viability of untreated cells at the time of administration was evaluated by adding 25 u L of CellTiter (ProMag catalog number G7573), a reagent for lysing cells and measuring total adenosine triphosphate (ATP) content. Incubate the plate at room temperature for 10 minutes to stabilize the luminescence signal before reading. Use luminous readingThe PHERAstar FSX ELISA reader (BMG Labtech) was used to measure the luminescence signals of all plates. This signal represents the cell viability of untreated cells on the day of administration or day 0.

   Click to Show/Hide
In Vitro Model Breast carcinoma ZR-75-30 cells CVCL_1661
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.09663 nM
High HER2 expression (HER2 +++)
Method Description
On the day of administration, HER2 targeted ADC and HER2 were prepared at a 10 fold ratio in standard growth medium. Add the prepared targeted ADC treatment to cells to obtain a final concentration of 3.81e-5nM to 100nM and a final volume of 50uL/well. Each drug concentration is tested in quadruplicate. On the same day, the cell viability of untreated cells at the time of administration was evaluated by adding 25 u L of CellTiter (ProMag catalog number G7573), a reagent for lysing cells and measuring total adenosine triphosphate (ATP) content. Incubate the plate at room temperature for 10 minutes to stabilize the luminescence signal before reading. Use luminous readingThe PHERAstar FSX ELISA reader (BMG Labtech) was used to measure the luminescence signals of all plates. This signal represents the cell viability of untreated cells on the day of administration or day 0.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma of no special type UACC812 cells CVCL_1781
Trastuzumab-Example 7 [Investigative]
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 (lC50)
0.1996 nM
High HER2 expression (HER2 +++)
Method Description
On the day of administration, HER2 targeted ADC and HER2 were prepared at a 10 fold ratio in standard growth medium. Add the prepared targeted ADC treatment to cells to obtain a final concentration of 3.81e-5nM to 100nM and a final volume of 50uL/well. Each drug concentration is tested in quadruplicate. On the same day, the cell viability of untreated cells at the time of administration was evaluated by adding 25 u L of CellTiter (ProMag catalog number G7573), a reagent for lysing cells and measuring total adenosine triphosphate (ATP) content. Incubate the plate at room temperature for 10 minutes to stabilize the luminescence signal before reading. Use luminous readingThe PHERAstar FSX ELISA reader (BMG Labtech) was used to measure the luminescence signals of all plates. This signal represents the cell viability of untreated cells on the day of administration or day 0.

   Click to Show/Hide
In Vitro Model Breast carcinoma ZR-75-30 cells CVCL_1661
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.6574 nM
High HER2 expression (HER2 +++)
Method Description
On the day of administration, HER2 targeted ADC and HER2 were prepared at a 10 fold ratio in standard growth medium. Add the prepared targeted ADC treatment to cells to obtain a final concentration of 3.81e-5nM to 100nM and a final volume of 50uL/well. Each drug concentration is tested in quadruplicate. On the same day, the cell viability of untreated cells at the time of administration was evaluated by adding 25 u L of CellTiter (ProMag catalog number G7573), a reagent for lysing cells and measuring total adenosine triphosphate (ATP) content. Incubate the plate at room temperature for 10 minutes to stabilize the luminescence signal before reading. Use luminous readingThe PHERAstar FSX ELISA reader (BMG Labtech) was used to measure the luminescence signals of all plates. This signal represents the cell viability of untreated cells on the day of administration or day 0.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma of no special type UACC812 cells CVCL_1781
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
1.888 nM
High HER2 expression (HER2 +++)
Method Description
On the day of administration, HER2 targeted ADC and HER2 were prepared at a 10 fold ratio in standard growth medium. Add the prepared targeted ADC treatment to cells to obtain a final concentration of 3.81e-5nM to 100nM and a final volume of 50uL/well. Each drug concentration is tested in quadruplicate. On the same day, the cell viability of untreated cells at the time of administration was evaluated by adding 25 u L of CellTiter (ProMag catalog number G7573), a reagent for lysing cells and measuring total adenosine triphosphate (ATP) content. Incubate the plate at room temperature for 10 minutes to stabilize the luminescence signal before reading. Use luminous readingThe PHERAstar FSX ELISA reader (BMG Labtech) was used to measure the luminescence signals of all plates. This signal represents the cell viability of untreated cells on the day of administration or day 0.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma BT-474 cells CVCL_0179
References
Ref 1 Antibody-drug conjugates