BAY 1135626
Based on 1 Customer Validation
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.19%
- CAS. Nr.: 1404071-37-9
- Formel: C55H86N10O11
- Molecular Weight:1063.33
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Speicherung:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Beschreibung
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. .
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Cell Line:hC4.4A:A549 lung cancer cells
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Concentration:0.001-100 nM
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Incubation Time:72 hours
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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.
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Cell Line:NCI-H292, FaDu, NCI-H322, SCaBER, SCC-4
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Concentration:0.001-100 nM
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Incubation Time:72 hours
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Result:Inhibited cancer cell growth in a dose-dependent manner.
In Vivo
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.
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Animal Model:C4.4A-positive NCI-H292 NSCLC xenograft mouse model[1]
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Dosage:1.9, 3.75, 7.5 mg/kg
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Administration:Intravenous injection; 20 days
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Result:Halted tumor growth on day 20 dose dependently, as the monotherapy treatment, with a minimum effective dose (MED) of 1.9 mg/kg.
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Animal Model:C4.4A-positive NCI-H292 NSCLC xenograft mouse model[1]
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Dosage:15 mg/kg
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Administration:Intravenous injection; 21 days for the first cycle teament, 57 days for the second cycle treatment
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Result:Reduced tumor volume with a marked delay of tumor growth.
Demonstrated well tolerance, still left regrown tumors sensitive to treatment.
Chemical Information
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CAS. Nr. 1404071-37-9
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Appearance Solid
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Molecular Weight 1063.33
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Formel C55H86N10O11
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Color White to off-white
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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
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Lösungsmittel & Löslichkeit
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)
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
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.
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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Reinheit & Dokumentation
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Data Sheet (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
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 |
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| 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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