1. MAPK/ERK Pathway
    Protein Tyrosine Kinase/RTK
    Apoptosis
  2. Raf
    Src
    Apoptosis
  3. CCT241161

CCT241161 

Cat. No.: HY-12847
Handling Instructions

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.

CCT241161 Chemical Structure

CCT241161 Chemical Structure

CAS No. : 1163719-91-2

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Description

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[1].

IC50 & Target

CRAF

6 nM (IC50)

Braf

30 nM (IC50)

BRafV600E

15 nM (IC50)

SRC

0.01 μM (IC50)

LCK

0.003 μM (IC50)

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].

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].

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.
Molecular Weight

541.62

Formula

C28H27N7O3S

CAS No.
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

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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CCT241161
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HY-12847
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