CCT241161
Based on 1 Customer Validation
CCT241161 is an orally active pan-RAF inhibitor with IC50s of 3, 6, 10, 15 and 30 nM for LCK, CRAF, SRC, V600E-BRAF and BRAF, respectively. CCT241161 shows good activity to in BRAF and NRAS mutant melanomas. CCT241161 also exhibits anticancer cell proliferative activity.
For research use only. We do not sell to patients.
- Purity : 99.77%
- CAS No.: 1163719-91-2
- Formula: C28H27N7O3S
- Molecular Weight:541.62
-
Storage: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]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
HY-14660
DabrafenibBRAF Inhibitor -
HY-15246
TovorafenibRaf Kinase Inhibitor -
HY-12558
LY3009120Pan RAF Inhibitor -
HY-18972
PlixorafenibBRAF Inhibitor -
HY-10966
SB-590885BRAF/c-Raf Inhibitor -
HY-11004
AZ 628Apoptosis Inducer -
HY-109080
BelvarafenibRAF Inhibitor -
HY-14660A
Dabrafenib MesylateRaf Inhibitor -
HY-13805
PP2Src Inhibitor -
HY-12846
CCT196969Raf Inhibitor -
HY-112089
NaporafenibB/CRAF Inhibitor -
HY-18227
B-Raf IN 1Raf Inhibitor
Biological Activity
Description
IC50 & Target
|
CRAF 6 nM (IC50) |
Braf 30 nM (IC50) |
BRafV600E 15 nM (IC50) |
SRC 0.01 μM (IC50) |
LCK 0.003 μM (IC50) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
10 nM
Compound: 15; CCT241161
|
Cytotoxicity against human A375 cells harboring BRAF V600E mutant after 72 hrs by CellTiter-Glo assay
Cytotoxicity against human A375 cells harboring BRAF V600E mutant after 72 hrs by CellTiter-Glo assay
|
[PMID: 29461827] |
In Vitro
CCT241161 (1, 3, 10, 30, 100 nM; 24 h) inhibits MEK and ERK in WM266.4 cells[1].
CCT241161 (1, 10, 100 nM and 1, 10, 100 µM) inhibits BRAFV600E in Ba/F3 cells[1].
CCT241161 (0.5 µM; 20 days) inhibits A375 cell but not cause drug resistance[1].
CCT241161 (1 µM , 4 h) inhibits BRAF-inhibitor-resistant melanoma cells[1].
CCT241161 (0.1, 0.3, 1, 3, 10 µM; 24 h) inhibits MEK in NRAS mutant cells[1].
CCT241161 (0.1, 1, 10, 100 µM) shows anti-proliferative activity in D04 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:WM266.4 cells (BRAF mutant)
-
Concentration:1, 3, 10, 30, 100 nM
-
Incubation Time:24 h
-
Result:Exhibited effects of inhibiting MEK and ERK in WM266.4 cells.
-
Cell Line:Ba/F3 cells
-
Concentration:1, 10, 100 nM and 1, 10, 100 µM
-
Incubation Time:
-
Result:Inhibited BRAF-V600E and BRAF-T529N, V600E in Ba/F3 cells.
-
Cell Line:A375 cell
-
Concentration:0.5 µM
-
Incubation Time:20 days
-
Result:Maintained inhibitory activity against A375 cell ,without drug resistance in 20 days.
-
Cell Line:D04 cells
-
Concentration:0.1, 1, 10, 100 µM
-
Incubation Time:
-
Result:Efficiently inhibited NRAS mutant cell growth.
-
Cell Line:patient #2 (PLX4720-resistant cells from patient with vemurafenib-resistant melanoma)
-
Concentration:1 µM
-
Incubation Time:4 h
-
Result:Inhibited MEK, ERK, and SRC in the cells from patient #2.
-
Cell Line:D04 cells
-
Concentration:0.1, 0.3, 1, 3, 10 µM
-
Incubation Time:24 h
-
Result:Showed activity of surpressing MEK in NRAS mutant cells.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Female nude mice (5 to 6- week-old)[1].
-
Dosage:10, 20 mg/kg
-
Administration:Oral gavage; once a day for 7 days.
-
Result:Showed activity of tumor regression in nude mice with xenografts tumor of BRAF mutant A375, PLX4720-resistant A375 (A375/R) and NRAS mutant DO4, without causing any body weight loss to the mice.
Chemical Information
-
CAS No. 1163719-91-2
-
Appearance Solid
-
Molecular Weight 541.62
-
Formula C28H27N7O3S
-
Color Light yellow to yellow
-
SMILES
O=C1C=NC2=C(N1)N=CC=C2OC3=CC=C(C(SC)=C3)NC(NC4=CC(C(C)(C)C)=NN4C5=CC=CC=C5)=O
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 50 mg/mL (92.32 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: 1.25 mg/mL (2.31 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 1.25 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: 1.25 mg/mL (2.31 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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:
-
-
-
-
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.
Purity & Documentation
-
Data Sheet (283 KB)
-
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)
-
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. 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 | 1.8463 mL | 9.2316 mL | 18.4631 mL | 46.1578 mL |
| 5 mM | 0.3693 mL | 1.8463 mL | 3.6926 mL | 9.2316 mL | |
| 10 mM | 0.1846 mL | 0.9232 mL | 1.8463 mL | 4.6158 mL | |
| 15 mM | 0.1231 mL | 0.6154 mL | 1.2309 mL | 3.0772 mL | |
| 20 mM | 0.0923 mL | 0.4616 mL | 0.9232 mL | 2.3079 mL | |
| 25 mM | 0.0739 mL | 0.3693 mL | 0.7385 mL | 1.8463 mL | |
| 30 mM | 0.0615 mL | 0.3077 mL | 0.6154 mL | 1.5386 mL | |
| 40 mM | 0.0462 mL | 0.2308 mL | 0.4616 mL | 1.1539 mL | |
| 50 mM | 0.0369 mL | 0.1846 mL | 0.3693 mL | 0.9232 mL | |
| 60 mM | 0.0308 mL | 0.1539 mL | 0.3077 mL | 0.7693 mL | |
| 80 mM | 0.0231 mL | 0.1154 mL | 0.2308 mL | 0.5770 mL |
CCT241161 Related Classifications
HY-12847 Related Classifications
Powered by Bioz