Bezuclastinib

Bezuclastinib
Clinical data
Other names	CGT-9486, PLX-9486
Legal status
Legal status	Investigational;
Identifiers
	IUPAC name 4,5-dimethyl-N-(2-phenyl-1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazole-3-carboxamide;
CAS Number	1616385-51-3;
PubChem CID	75593308;
IUPHAR/BPS	11868;
DrugBank	DB18041;
ChemSpider	115007996;
UNII	2ROQ545LAG;
KEGG	D12600;
ChEMBL	ChEMBL5095229;
PDB ligand	WEJ (PDBe, RCSB PDB);
Chemical and physical data
Formula	C19H17N5O
Molar mass	331.379 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC1=C(NN=C1C(=O)NC2=CN=C3C(=C2)C=C(N3)C4=CC=CC=C4)C;
	InChI InChI=1S/C19H17N5O/c1-11-12(2)23-24-17(11)19(25)21-15-8-14-9-16(22-18(14)20-10-15)13-6-4-3-5-7-13/h3-10H,1-2H3,(H,20,22)(H,21,25)(H,23,24); Key:NVSHVYGIYPBTEZ-UHFFFAOYSA-N;

Bezuclastinib is an investigational new drug that is being evaluated for the treatment of solid tumors and systemic mastocytosis.^[1]^[2] It acts as an inhibitor of KIT (a specific type of receptor tyrosine kinase).^[3]

References

↑ "Bezuclastinib - Cogent Biosciences". AdisInsight. Springer Nature Switzerland AG.
↑ Farmer I, Radia DH (August 2024). "Systemic Mastocytosis: State of the Art". Current Hematologic Malignancy Reports. doi:10.1007/s11899-024-00737-8. PMID 39187708.
↑ Wagner AJ, Severson PL, Shields AF, Patnaik A, Chugh R, Tinoco G, et al. (September 2021). "Association of Combination of Conformation-Specific KIT Inhibitors With Clinical Benefit in Patients With Refractory Gastrointestinal Stromal Tumors: A Phase 1b/2a Nonrandomized Clinical Trial". JAMA Oncology. 7 (9): 1343–1350. doi:10.1001/jamaoncol.2021.2086. PMC 8267845. PMID 34236401.

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[1] "Bezuclastinib - Cogent Biosciences". AdisInsight. Springer Nature Switzerland AG.

[Farmer_2024-2] Farmer I, Radia DH (August 2024). "Systemic Mastocytosis: State of the Art". Current Hematologic Malignancy Reports. doi:10.1007/s11899-024-00737-8. PMID 39187708.

[Wagner_2021-3] Wagner AJ, Severson PL, Shields AF, Patnaik A, Chugh R, Tinoco G, et al. (September 2021). "Association of Combination of Conformation-Specific KIT Inhibitors With Clinical Benefit in Patients With Refractory Gastrointestinal Stromal Tumors: A Phase 1b/2a Nonrandomized Clinical Trial". JAMA Oncology. 7 (9): 1343–1350. doi:10.1001/jamaoncol.2021.2086. PMC 8267845. PMID 34236401.

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