Belvarafenib

Belvarafenib
Clinical data
Other names	HM95573 GDC5573 RG6185
Routes of; administration	By mouth
Identifiers
	IUPAC name 4-amino-N-[1-(3-chloro-2-fluoroanilino)-6-methylisoquinolin-5-yl]thieno[3,2-d]pyrimidine-7-carboxamide;
CAS Number	1446113-23-0;
PubChem CID	89655386;
IUPHAR/BPS	11544;
ChemSpider	64878400;
UNII	31M3WLJ3KG;
ChEMBL	ChEMBL3977543;
Chemical and physical data
Formula	C23H16ClFN6OS
Molar mass	478.93 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC1=C(C2=C(C=C1)C(=NC=C2)NC3=C(C(=CC=C3)Cl)F)NC(=O)C4=CSC5=C4N=CN=C5N;
	InChI InChI=InChI=1S/C23H16ClFN6OS/c1-11-5-6-13-12(7-8-27-22(13)30-16-4-2-3-15(24)17(16)25)18(11)31-23(32)14-9-33-20-19(14)28-10-29-21(20)26/h2-10H,1H3,(H,27,30)(H,31,32)(H2,26,28,29); Key:KVCQTKNUUQOELD-UHFFFAOYSA-N;

Belvarafenib (developed by Hanmi Pharmaceuticals and Genentech) is a small molecule RAF dimer (type II) inhibitor^[1] which shows anti-tumor clinical activity in cancer patients with BRAFV600E- and NRAS- mutations.^[2]

References

^ Awada G, Neyns B (March 2022). "Melanoma with genetic alterations beyond the BRAFV600 mutation: management and new insights". Current Opinion in Oncology. 34 (2): 115–122. doi:10.1097/CCO.0000000000000817. PMID 35050937.
^ Kim TW, Lee J, Shin SJ, Kim JS, Kim YJ, Han HS, Lee SJ, Lim HS, Hong YH, Noh YS, Kyoung Y (31 May 2019). "Belvarafenib, a novel pan-RAF inhibitor, in solid tumor patients harboring BRAF, KRAS, or NRAS mutations: Phase I study". Journal of Clinical Oncology. 37 (15 suppl): 3000. doi:10.1200/JCO.2019.37.15_suppl.3000.

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Clinical data

Other names	HM95573 GDC5573 RG6185
Routes of administration	By mouth
Identifiers
IUPAC name 4-amino-N-[1-(3-chloro-2-fluoroanilino)-6-methylisoquinolin-5-yl]thieno[3,2-d]pyrimidine-7-carboxamide
CAS Number	1446113-23-0
PubChem CID	89655386
IUPHAR/BPS	11544
ChemSpider	64878400
UNII	31M3WLJ3KG
ChEMBL	ChEMBL3977543
Chemical and physical data
Formula	C₂₃H₁₆ClFN₆OS
Molar mass	478.93 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES CC1=C(C2=C(C=C1)C(=NC=C2)NC3=C(C(=CC=C3)Cl)F)NC(=O)C4=CSC5=C4N=CN=C5N
InChI InChI=InChI=1S/C23H16ClFN6OS/c1-11-5-6-13-12(7-8-27-22(13)30-16-4-2-3-15(24)17(16)25)18(11)31-23(32)14-9-33-20-19(14)28-10-29-21(20)26/h2-10H,1H3,(H,27,30)(H,31,32)(H2,26,28,29) Key:KVCQTKNUUQOELD-UHFFFAOYSA-N