CCT241161 

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].

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.

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.

541.62

C₂₈H₂₇N₇O₃S

1163719-91-2

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

Room temperature in continental US; may vary elsewhere.

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

• [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]