产品
编 号：F601993
分子式：C28H27N7O3S
分子量：541.62
分子式：C28H27N7O3S
分子量：541.62
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CAS No: 1163719-91-2
产品详情
生物活性：
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.
体内研究：
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.Animal Model:Female nude mice (5 to 6- week-old).
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.
体外研究：
CCT241161 (1, 3, 10, 30, 100 nM; 24 h) inhibits MEK and ERK in WM266.4 cells.CCT241161 (1, 10, 100 nM and 1, 10, 100 μM) inhibits BRAFV600E in Ba/F3 cells.CCT241161 (0.5 μM; 20 days) inhibits A375 cell but not cause drug resistance.CCT241161 (1 μM , 4 h) inhibits BRAF-inhibitor-resistant melanoma cells.CCT241161 (0.1, 0.3, 1, 3, 10 μM; 24 h) inhibits MEK in NRAS mutant cells.CCT241161 (0.1, 1, 10, 100 μM) shows anti-proliferative activity in D04 cells.
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.
体内研究：
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.Animal Model:Female nude mice (5 to 6- week-old).
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.
体外研究：
CCT241161 (1, 3, 10, 30, 100 nM; 24 h) inhibits MEK and ERK in WM266.4 cells.CCT241161 (1, 10, 100 nM and 1, 10, 100 μM) inhibits BRAFV600E in Ba/F3 cells.CCT241161 (0.5 μM; 20 days) inhibits A375 cell but not cause drug resistance.CCT241161 (1 μM , 4 h) inhibits BRAF-inhibitor-resistant melanoma cells.CCT241161 (0.1, 0.3, 1, 3, 10 μM; 24 h) inhibits MEK in NRAS mutant cells.CCT241161 (0.1, 1, 10, 100 μM) shows anti-proliferative activity in D04 cells.
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