Linker Information

General Information of This Linker
Linker ID
LIN0SGYVK
Linker Name
CN119343152A Trastuzumab-Example8 Linker
Linker Type
Cathepsin-cleavable linker
Antibody-Linker Relation
Cleavable
Structure
Formula
C188H343N19O87P2
Isosmiles
CN(C(CN(CC(N(C)CCOCCOCCOCCC(N[C@@H](C(C)C)C(N[C@H](C(NC1=CC=C(COP(O)(O)=O)C(CN(C(NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCC(O)=O)=O)C)=C1)=O)CCCNC(N)=O)=O)=O)=O)C(CCOCCNC(CCOCCOCCOCCOCCN2C(C=CC2=O)=O)=O)=O)=O)CCOCCOCCOCCC(N[C@@H](C(C)C)C(N[C@H](C(NC(C=C3CN(C(NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCC(O)=O)=O)C)=CC=C3COP(O)(O)=O)=O)CCCNC(N)=O)=O)=O
InChI
InChI=1S/C188H343N19O87P2/c1-159(2)179(183(222)198-167(11-9-25-192-185(189)224)181(220)196-165-15-13-161(157-293-295(228,229)230)163(151-165)153-204(7)187(226)194-28-40-240-50-60-250-68-73-255-77-81-259-85-89-263-93-97-267-101-105-271-109-113-275-117-121-279-125-129-283-133-137-287-141-145-291-149-147-289-143-139-285-135-131-281-127-123-277-119-115-273-111-107-269-103-99-265-95-91-261-87-83-257-79-75-253-71-66-248-58-48-238-37-23-177(216)217)200-170(209)20-34-236-46-56-245-62-52-242-42-30-202(5)175(214)155-206(172(211)22-36-234-39-27-191-169(208)19-33-235-45-55-247-65-70-252-64-54-244-44-32-207-173(212)17-18-174(207)213)156-176(215)203(6)31-43-243-53-63-246-57-47-237-35-21-171(210)201-180(160(3)4)184(223)199-168(12-10-26-193-186(190)225)182(221)197-166-16-14-162(158-294-296(231,232)233)164(152-166)154-205(8)188(227)195-29-41-241-51-61-251-69-74-256-78-82-260-86-90-264-94-98-268-102-106-272-110-114-276-118-122-280-126-130-284-134-138-288-142-146-292-150-148-290-144-140-286-136-132-282-128-124-278-120-116-274-112-108-270-104-100-266-96-92-262-88-84-258-80-76-254-72-67-249-59-49-239-38-24-178(218)219/h13-18,151-152,159-160,167-168,179-180H,9-12,19-150,153-158H2,1-8H3,(H,191,208)(H,194,226)(H,195,227)(H,196,220)(H,197,221)(H,198,222)(H,199,223)(H,200,209)(H,201,210)(H,216,217)(H,218,219)(H3,189,192,224)(H3,190,193,225)(H2,228,229,230)(H2,231,232,233)/t167-,168-,179-,180-/m0/s1
InChIKey
OBGALJZIUUOVTH-CDBSKEOLSA-N
Pharmaceutical Properties
Molecule Weight
4323.806
Polar area
1229.62
Complexity
.
xlogp Value
-1.8108
Heavy Count
296
Rot Bonds
229
Hbond acc
81
Hbond Donor
19
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
Trastuzumab-Example 8 [Investigative]
 ADC Info 
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)
0.239 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 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)
1.892 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)
4.991 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