Naporafenib(LXH-254) - 半岛电竞官方网址

	Name: LXH254 CAS#: 1800398-38-2 (free base) Chemical Formula: C25H25F3N4O4 Exact Mass: 502.1828 Molecular Weight: 502.4942
Storage	-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Technical Information	Synonym: LXH-254; Naporafenib; LXH254; LXH 254 Chemical Name: N-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide InChi Key: UEPXBTCUIIGYCY-UHFFFAOYSA-N InChi Code: InChI=1S/C25H25F3N4O4/c1-16-2-3-19(30-24(34)17-4-5-29-21(12-17)25(26,27)28)15-20(16)18-13-22(32-6-9-35-10-7-32)31-23(14-18)36-11-8-33/h2-5,12-15,33H,6-11H2,1H3,(H,30,34) SMILES Code: O=C(C1=CC(C(F)(F)F)=NC=C1)NC2=CC=C(C)C(C3=CC(OCCO)=NC(N4CCOCC4)=C3)=C2

Name: LXH254
CAS#: 1800398-38-2 (free base)
Chemical Formula: C25H25F3N4O4
Exact Mass: 502.1828
Molecular Weight: 502.4942

Storage

-20℃ for 3 years in powder form

-80℃ for 2 years in solvent

Technical Information

Synonym: LXH-254; Naporafenib; LXH254; LXH 254
Chemical Name: N-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide
InChi Key: UEPXBTCUIIGYCY-UHFFFAOYSA-N
InChi Code: InChI=1S/C25H25F3N4O4/c1-16-2-3-19(30-24(34)17-4-5-29-21(12-17)25(26,27)28)15-20(16)18-13-22(32-6-9-35-10-7-32)31-23(14-18)36-11-8-33/h2-5,12-15,33H,6-11H2,1H3,(H,30,34)
SMILES Code: O=C(C1=CC(C(F)(F)F)=NC=C1)NC2=CC=C(C)C(C3=CC(OCCO)=NC(N4CCOCC4)=C3)=C2

Target	Braf; c-Raf
In Vitro	LXH254 (Compound A) is an adenosine triphosphate (ATP)-competitive inhibitor of BRAF (also referred to herein as b-RAF or b-Raf) and CRAF (also referred to herein as c-RAF or c- Raf) protein kinases. Throughout the present disclosure, LXH254 is also referred to as a c-RAF (or CRAF) inhibitor or a C-RAF/c-Raf kinase inhibitor. In cell-based assays, LXH254 has demonstrated anti-proliferative activity in cell lines that contain a variety of mutations that activate MAPK signaling. Moreover, LXH254 is a Type 2 ATP -competitive inhibitor of both B-Raf and C-Raf that keeps the kinase pocket in an inactive conformation, thereby reducing the paradoxical activation seen with many B-Raf inhibitors, and blocking mutant RAS-driven signaling and cell proliferation[1].
In Vivo	Treatment with LXH254 (Compound A) generates tumor regression in several KRAS-mutant models including the NSCLC-derived Calu-6 (KRAS Q61K) and NCI-H358 (KRAS G12C). LXH254 exhibits efficacy in numerous MAPK-driven human cancer cell lines and in xenograft tumors representing model tumors harboring human lesions in KRAS, NRAS and BRAF oncogenes[1].
References	WO 2018051306 A1 20180322; /13_Supplement/DDT01-04

Target

Braf; c-Raf

In Vitro

LXH254 (Compound A) is an adenosine triphosphate (ATP)-competitive inhibitor of BRAF (also referred to herein as b-RAF or b-Raf) and CRAF (also referred to herein as c-RAF or c- Raf) protein kinases. Throughout the present disclosure, LXH254 is also referred to as a c-RAF (or CRAF) inhibitor or a C-RAF/c-Raf kinase inhibitor. In cell-based assays, LXH254 has demonstrated anti-proliferative activity in cell lines that contain a variety of mutations that activate MAPK signaling. Moreover, LXH254 is a Type 2 ATP -competitive inhibitor of both B-Raf and C-Raf that keeps the kinase pocket in an inactive conformation, thereby reducing the paradoxical activation seen with many B-Raf inhibitors, and blocking mutant RAS-driven signaling and cell proliferation[1].

In Vivo

Treatment with LXH254 (Compound A) generates tumor regression in several KRAS-mutant models including the NSCLC-derived Calu-6 (KRAS Q61K) and NCI-H358 (KRAS G12C). LXH254 exhibits efficacy in numerous MAPK-driven human cancer cell lines and in xenograft tumors representing model tumors harboring human lesions in KRAS, NRAS and BRAF oncogenes[1].

References

WO 2018051306 A1 20180322; /13_Supplement/DDT01-04

CAS NO:	1800398-38-2
规格:	≥98%

包装	价格(元)
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议
250mg	电议