UNC9435
Based on 1 Customer Validation
UNC9435 is a TYRO3/MERTK receptor tyrosine kinase inhibitor with IC50 values of 3.7 nM and 1.1 nM, respectively. UNC9435 inhibits TYRO3/MERTK kinase activity and autophosphorylation. UNC9435 shows certain inhibitory activity against AXL, LCK, PDGFRα, and TRKA. UNC9435 inhibits PROS1 (HY-P74614)-stimulated downstream AKT signaling, macrophage efferocytosis, and colony formation. UNC9435 can be used in research related to non-small cell lung cancer.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.08%
- No. CAS: 3091640-25-1
- Fòrmula: C27H38ClN5O
- Peso molecular:484.08
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
[1]|
Tyro3 3.7 nM (IC50) |
MERTK 1.1 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H1650 | EC50 |
390 nM
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Inhibition of colony formation in human H1650 NSCLC cells assessed by crystal violet staining after 7 to 10 days incubation.
Inhibition of colony formation in human H1650 NSCLC cells assessed by crystal violet staining after 7 to 10 days incubation.
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40215328 |
| H1975 | EC50 |
900 nM
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Inhibition of colony formation in human H1975 NSCLC cells assessed by crystal violet staining after 7 to 10 days incubation.
Inhibition of colony formation in human H1975 NSCLC cells assessed by crystal violet staining after 7 to 10 days incubation.
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40215328 |
In Vitro
UNC9435 (300-1000 nM; 1.5 h) reduces PROS1 (HY-P74614)-stimulated AKT signaling in T11 mouse breast cancer cells[1].
UNC9435 (7-10 days) inhibits colony formation in H1650 and H1975 NSCLC cultures with EC50 values of 390 nM and 900 nM, respectively[1].
UNC9435 (110 nM) completely inhibits TYRO3 and MERTK, and inhibits AXL, LCK, PDGFRα, and TRKA, with no significant inhibitory effect on serine/threonine kinases[1].
UNC9435 binds to TYRO3 and MERTK in HEK293 cells, with EC50 values both <0.51 nM, and exhibits more than 3000-fold selectivity over AXL[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H4011 NSCLC cells
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Concentration:5, 10, 25, 50, 200, 500 and 250 nM
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Incubation Time:1.5 h
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Result:Dose-dependent inhibition of MERTK and TYRO3 autophosphorylation occurred in NSCLC cells at concentrations as low as 200-250 nM.
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Cell Line:T11 murine breast cancer cells
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Concentration:30, 100, 300, 500, 1000 and 3000 nM
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Incubation Time:1.5 h
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Result:AKT signaling downstream of PROS1 stimulation was reduced in T11 cells at concentrations similar to those inhibiting MERTK/TYRO3 autophosphorylation.
Parmacokinetics
| Species | Dose | Route | T1/2 | Cmax |
|---|---|---|---|---|
| Mice[1] | 10 mg/kg | i.p. | 2.5 h | 330 nM |
Chemical Information
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No. CAS 3091640-25-1
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Appearance Solid
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Peso molecular 484.08
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Fòrmula C27H38ClN5O
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Color White to off-white
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SMILES
O[C@H]1CC[C@H](NC2=NC(NC3=CC=CC(Cl)=C3)=NC=C2C4CCN(CC5CCCC5)CC4)CC1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (206.58 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. 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.5 mg/mL (5.16 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
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.
Pureza y Documentación
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Ficha de datos (275 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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. 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 | 2.0658 mL | 10.3289 mL | 20.6577 mL | 51.6444 mL |
| 5 mM | 0.4132 mL | 2.0658 mL | 4.1315 mL | 10.3289 mL | |
| 10 mM | 0.2066 mL | 1.0329 mL | 2.0658 mL | 5.1644 mL | |
| 15 mM | 0.1377 mL | 0.6886 mL | 1.3772 mL | 3.4430 mL | |
| 20 mM | 0.1033 mL | 0.5164 mL | 1.0329 mL | 2.5822 mL | |
| 25 mM | 0.0826 mL | 0.4132 mL | 0.8263 mL | 2.0658 mL | |
| 30 mM | 0.0689 mL | 0.3443 mL | 0.6886 mL | 1.7215 mL | |
| 40 mM | 0.0516 mL | 0.2582 mL | 0.5164 mL | 1.2911 mL | |
| 50 mM | 0.0413 mL | 0.2066 mL | 0.4132 mL | 1.0329 mL | |
| 60 mM | 0.0344 mL | 0.1721 mL | 0.3443 mL | 0.8607 mL | |
| 80 mM | 0.0258 mL | 0.1291 mL | 0.2582 mL | 0.6456 mL | |
| 100 mM | 0.0207 mL | 0.1033 mL | 0.2066 mL | 0.5164 mL |
UNC9435 Related Classifications
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