Art. -Nr.: HY-12847

CCT241161

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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.

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Reinheit: 99.77%
CAS. Nr.: 1163719-91-2
Formel: C₂₈H₂₇N₇O₃S
Molecular Weight:541.62

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

CCT241161 Chemical Structure

CAS. Nr.: 1163719-91-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

CRAF

6 nM (IC₅₀)

Braf

30 nM (IC₅₀)

BRaf^V600E

15 nM (IC₅₀)

SRC

0.01 μM (IC₅₀)

LCK

0.003 μM (IC₅₀)

Alle Raf Isoform-spezifische Produkte anzeigen :

Alle Src Isoform-spezifische Produkte anzeigen :

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 BRAF^V600E 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 Viability Assay^[1]

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 Viability Assay^[1]

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 Viability Assay^[1]

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 Proliferation Assay^[1]

Cell Line:

D04 cells
Concentration:

0.1, 1, 10, 100 µM
Incubation Time:
Result:

Efficiently inhibited NRAS mutant cell growth.

Western Blot Analysis^[1]

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.

Western Blot Analysis^[1]

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

CCT241161 (10, 20 mg/kg; i.g; once a day for 7 days) inhibits the growth of BRAF mutant A375, PLX4720-resistant A375 and NRAS mutant DO4 tumor xenografts in mice^[1].

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. Nr. 1163719-91-2
Appearance Solid
Molecular Weight 541.62
Formel 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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Girotti MR, et al. Paradox-breaking RAF inhibitors that also target SRC are effective in drug-resistant BRAF mutant melanoma. Cancer Cell. 2015 Jan 12;27(1):85-96. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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CCT241161

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Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cell Death Library

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Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Alle Raf Isoform-spezifische Produkte anzeigen

Alle Src Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

CCT241161 Related Classifications

HY-12847 Related Classifications