2. Antibody-drug Conjugate/ADC Related
  3. Drug-Linker Conjugates for ADC
  4. BAY 1135626

BAY 1135626 is used to synthesize BAY 1129980, and use to anti-tumor research. BAY 1129980 is a Auristatin-based anti-C4.4A (LYPD3) antibody–agent conjugate (ADC), is used to non–small cell lung cancer (NSCLC) research.

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BAY 1135626 Chemical Structure

BAY 1135626 Chemical Structure

CAS No. : 1404071-37-9

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Description

BAY 1135626 is used to synthesize BAY 1129980, and use to anti-tumor research. BAY 1129980 is a Auristatin-based anti-C4.4A (LYPD3) antibody–agent conjugate (ADC), is used to non–small cell lung cancer (NSCLC) research[1].

In Vitro

C4.4A (LYPD3) is a protein expressed in non-small cell lung cancer (NSCLC), with scarcely expressing in normal tissues[1].
BAY 1135626 can be synthesized into BAY 1129980 (C4.4A-ADC), shows a strong anti-proliferative effect on C4.4A expressing cell lines[1].
BAY 1129980 (0.001-100 nM; 72 h) inhibits the proliferation of A549 lung cancer cell lines transfected with C4.4A[1].
BAY 1129980 (0.001-100 nM; 72 h) exhibits high and selective efficacy on hC4.4A:A549 cells in vitro[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

BAY 1135626 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: hC4.4A:A549 lung cancer cells
Concentration: 0.001-100 nM
Incubation Time: 72 hours
Result: High potency at subnanomolar range with an IC50 value of 0.05 nM.
Resulted remarkable selectivity on hC4.4A:A549 with over 1,000-fold compared with mock:A549 cells.

Cell Viability Assay[1]

Cell Line: NCI-H292, FaDu, NCI-H322, SCaBER, SCC-4
Concentration: 0.001-100 nM
Incubation Time: 72 hours
Result: Inhibited cancer cell growth in a dose-dependent manner.
In Vivo

BAY 1129980 (1.9-7.5 mg/kg; i.v.; 20 d) inhibits tumor growth in vivo in mouse[1].
BAY 1129980 with a repeated dosing (15 mg/kg; i.v.; 21 d for 1st cycle and 57 d for 2nd cycle) is well tolerated without changing the sensitivity to the treatment[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C4.4A-positive NCI-H292 NSCLC xenograft mouse model[1]
Dosage: 1.9, 3.75, 7.5 mg/kg
Administration: Intravenous injection; 20 days
Result: Halted tumor growth on day 20 dose dependently, as the monotherapy treatment, with a minimum effective dose (MED) of 1.9 mg/kg.
Animal Model: C4.4A-positive NCI-H292 NSCLC xenograft mouse model[1]
Dosage: 15 mg/kg
Administration: Intravenous injection; 21 days for the first cycle teament, 57 days for the second cycle treatment
Result: Reduced tumor volume with a marked delay of tumor growth.
Demonstrated well tolerance, still left regrown tumors sensitive to treatment.
Molecular Weight

1063.33

Formula

C55H86N10O11
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CO[C@@H]([C@@]1([H])N(CCC1)C(C[C@@H](OC)[C@H]([C@@H](C)CC)N(C)C([C@H](C(C)C)NC([C@H](C(C)C)N(C)CCCC(NNC(CCCCCN2C(C=CC2=O)=O)=O)=O)=O)=O)=O)[C@@H](C)C(N[C@H](C(N)=O)CC3=CNC4=CC=CC=C34)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (94.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9404 mL 4.7022 mL 9.4044 mL
5 mM 0.1881 mL 0.9404 mL 1.8809 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 3.5 mg/mL (3.29 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (35.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 3.5 mg/mL (3.29 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (35.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.19%

SDS (251 KB)

COA (246 KB) HNMR (383 KB) RP-HPLC (264 KB) LCMS (106 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.9404 mL 4.7022 mL 9.4044 mL 23.5110 mL
5 mM 0.1881 mL 0.9404 mL 1.8809 mL 4.7022 mL
10 mM 0.0940 mL 0.4702 mL 0.9404 mL 2.3511 mL
15 mM 0.0627 mL 0.3135 mL 0.6270 mL 1.5674 mL
20 mM 0.0470 mL 0.2351 mL 0.4702 mL 1.1756 mL
25 mM 0.0376 mL 0.1881 mL 0.3762 mL 0.9404 mL
30 mM 0.0313 mL 0.1567 mL 0.3135 mL 0.7837 mL
40 mM 0.0235 mL 0.1176 mL 0.2351 mL 0.5878 mL
50 mM 0.0188 mL 0.0940 mL 0.1881 mL 0.4702 mL
60 mM 0.0157 mL 0.0784 mL 0.1567 mL 0.3919 mL
80 mM 0.0118 mL 0.0588 mL 0.1176 mL 0.2939 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BAY 11356261404071-37-9BAY1135626BAY-1135626Drug-Linker Conjugates for ADCnon–small cell lung cancerNSCLCBAY 1129980anti-tumorC4.4A-ADCantibody–drug conjugateAuristatinLYPD3Inhibitorinhibitorinhibit

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