Crelosidenib

Crelosidenib
Clinical data
Other names	LY3410738
Identifiers
	IUPAC name 7-[[(1S)-1-[4-[(1S)-2-cyclopropyl-1-(4-prop-2-enoylpiperazin-1-yl)ethyl]phenyl]ethyl]amino]-1-ethyl-4H-pyrimido[4,5-d][1,3]oxazin-2-one;
CAS Number	2230263-60-0;
PubChem CID	135125140;
IUPHAR/BPS	12340;
ChemSpider	115009279;
UNII	A4DU555RMD;
KEGG	D12708;
Chemical and physical data
Formula	C28H36N6O3
Molar mass	504.635 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CCN1C2=NC(=NC=C2COC1=O)N[C@@H](C)C3=CC=C(C=C3)[C@H](CC4CC4)N5CCN(CC5)C(=O)C=C;
	InChI InChI=InChI=1S/C28H36N6O3/c1-4-25(35)33-14-12-32(13-15-33)24(16-20-6-7-20)22-10-8-21(9-11-22)19(3)30-27-29-17-23-18-37-28(36)34(5-2)26(23)31-27/h4,8-11,17,19-20,24H,1,5-7,12-16,18H2,2-3H3,(H,29,30,31)/t19-,24-/m0/s1; Key:AFGYODUJVVOZAX-CYFREDJKSA-N;

Crelosidenib is an investigational new drug that is being evaluated for the treatment of cancer. It acts as a selective inhibitor of isocitrate dehydrogenase 1 (IDH1), an enzyme that plays a crucial role in cellular metabolism and is frequently mutated in various cancers, including cholangiocarcinoma.^[1]^[2]

References

^ Zarei M, Hue JJ, Hajihassani O, Graor HJ, Katayama ES, Loftus AW, et al. (February 2022). "Clinical development of IDH1 inhibitors for cancer therapy". Cancer Treatment Reviews. 103: 102334. doi:10.1016/j.ctrv.2021.102334. PMID 34974243.
^ Demir T, Moloney C, Mahalingam D (July 2024). "Emerging targeted therapies and strategies to overcome resistance in biliary tract cancers". Critical Reviews in Oncology/Hematology. 199: 104388. doi:10.1016/j.critrevonc.2024.104388. PMID 38754771.

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[Zarei_2022-1] Zarei M, Hue JJ, Hajihassani O, Graor HJ, Katayama ES, Loftus AW, et al. (February 2022). "Clinical development of IDH1 inhibitors for cancer therapy". Cancer Treatment Reviews. 103: 102334. doi:10.1016/j.ctrv.2021.102334. PMID 34974243.

[Demir_2024-2] Demir T, Moloney C, Mahalingam D (July 2024). "Emerging targeted therapies and strategies to overcome resistance in biliary tract cancers". Critical Reviews in Oncology/Hematology. 199: 104388. doi:10.1016/j.critrevonc.2024.104388. PMID 38754771.

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