Darovasertib
Based on 4 publication(s) in Google Scholar
Darovasertib (LXS196) is a potent, selective and orally active protein kinase C (PKC) inhibitor, with IC50 values of 1.9 nM, 0.4 nM and 3.1 μM for PKCα, PKCθ and GSK3β, respectively. Darovasertib has the potential for uveal melanoma research.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.78%
- No. CAS: 1874276-76-2
- Fòrmula: C22H23F3N8O
- Peso molecular:472.47
-
Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Darovasertib
More
Customer Validation & Images
-
Cell Proliferation/Viability Assay
-
Cell Proliferation/Viability Assay
Actividad biológica
Descripciòn
IC50 & Target
[2]|
PKCα 1.9 nM (IC50) |
PKCθ 0.4 nM (IC50) |
GSK3β 3.1 μM (IC50) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| SK-MEL-28 | IC50 |
>10 μM
Compound: 20; LXS196
|
Cytotoxicity against human SK-MEL-28 cells expressing B-Raf V600E mutant
Cytotoxicity against human SK-MEL-28 cells expressing B-Raf V600E mutant
|
[PMID: 38198520] |
In Vitro
Upon oral administration, protein kinase C inhibitor Darovasertib (LXS196) binds to and inhibits PKC, which prevents the activation of PKC-mediated signaling pathways. This may lead to the induction of cell cycle arrest and apoptosis in susceptible tumor cells. PKC, a serine/threonine protein kinase overexpressed in certain types of cancer cells, is involved in tumor cell differentiation, proliferation, invasion and survival[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Mice implanted with 92.1 GNAQ mutant uveal melanoma cells[2].
-
Dosage:15, 30, 75, 150 mg/kg
-
Administration:P.O. (bid) for 35 days
-
Result:Dose-dependently suppressed the tumor growth.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
No. CAS 1874276-76-2
-
Appearance Solid
-
Peso molecular 472.47
-
Fòrmula C22H23F3N8O
-
Color Light yellow to yellow
-
SMILES
NC1=C(C(NC2=C(N3CCC(C)(N)CC3)C=CC=N2)=O)N=C(C4=NC=CC=C4C(F)(F)F)C=N1
-
Synonyms
LXS196; IDE196
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
-
Journal Impact Factor
-
Most Recent
-
Nat Commun
Signature-driven repurposing of Midostaurin for combination with MEK1/2 and KRASG12C inhibitors in lung cancer. [Abstract]2023 Oct 10;14(1):6332. PMID: 37816716 -
Cancers (Basel)
FAK Inhibitor-Based Combinations with MEK or PKC Inhibitors Trigger Synergistic Antitumor Effects in Uveal Melanoma. [Abstract]2023 Apr 13;15(8):2280. PMID: 37190207 -
-
Darovasertib purchased from MedChemExpress. Usage Cited in: Patent. US20210230154A1.
Darovasertib (0-10 μM) inhibited 92-1 cells growth in a dose-dependent manner.
Darovasertib purchased from MedChemExpress. Usage Cited in: Patent. US20210230154A1.
Darovasertib (0-10 μM) inhibited MP-14 cells growth in a dose-dependent manner.
Solvente y solubilidad
In Vitro:
DMSO : 25 mg/mL (52.91 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 (5.29 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.29 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 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.
Add each solvent one by one: 1% DMSO 99% Saline
Solubility: 0.33 mg/mL (0.70 mM); Suspended solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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
-
Ficha de datos (278 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1165 mL | 10.5827 mL | 21.1654 mL | 52.9134 mL |
| 5 mM | 0.4233 mL | 2.1165 mL | 4.2331 mL | 10.5827 mL | |
| 10 mM | 0.2117 mL | 1.0583 mL | 2.1165 mL | 5.2913 mL | |
| 15 mM | 0.1411 mL | 0.7055 mL | 1.4110 mL | 3.5276 mL | |
| 20 mM | 0.1058 mL | 0.5291 mL | 1.0583 mL | 2.6457 mL | |
| 25 mM | 0.0847 mL | 0.4233 mL | 0.8466 mL | 2.1165 mL | |
| 30 mM | 0.0706 mL | 0.3528 mL | 0.7055 mL | 1.7638 mL | |
| 40 mM | 0.0529 mL | 0.2646 mL | 0.5291 mL | 1.3228 mL | |
| 50 mM | 0.0423 mL | 0.2117 mL | 0.4233 mL | 1.0583 mL |
Darovasertib Related Classifications
HY-101569 Related Classifications
Powered by Bioz