Sapanisertib

Sapanisertib
Identifiers
	IUPAC name 5-(4-Amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)-1,3-benzoxazol-2-amine;
CAS Number	1224844-38-5;
PubChem CID	45375953;
KEGG	D11183;
Chemical and physical data
Formula	C15H15N7O
Molar mass	309.333 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC(C)N1C2=C(C(=N1)C3=CC4=C(C=C3)OC(=N4)N)C(=NC=N2)N;
	InChI InChI=1S/C15H15N7O/c1-7(2)22-14-11(13(16)18-6-19-14)12(21-22)8-3-4-10-9(5-8)20-15(17)23-10/h3-7H,1-2H3,(H2,17,20)(H2,16,18,19); Key:GYLDXIAOMVERTK-UHFFFAOYSA-N;

Sapanisertib (also known as INK128 and TAK-228) is an experimental small molecule inhibitor of mTOR which is administered orally. It targets both mTORC1 and mTORC2.[1]

Developed by Millennium Pharmaceuticals,[2] sapanisertib is in phase II clinical trials for breast cancer, endometrial cancer, glioblastoma, renal cell carcinoma, and thyroid cancer.[3] The drug has been well tolerated by patients with advanced solid tumours in Phase I trials.[4]

References

"sapanisertib". NCI Drug Dictionary. National Cancer Institute. 2 February 2011. Retrieved 23 August 2019.
https://searchusan.ama-assn.org/usan/documentDownload?uri=%2Funstructured%2Fbinary%2Fusan%2Fsapanisertib.pdf
http://adisinsight.springer.com/drugs/800030541
Moore, Kathleen N; Bauer, Todd M; Falchook, Gerald S; Chowdhury, Swapan; Patel, Chirag; Neuwirth, Rachel; Enke, Aaron; Zohren, Fabian; Patel, Manish R (February 2018). "Phase I study of the investigational oral mTORC1/2 inhibitor sapanisertib (TAK-228): tolerability and food effects of a milled formulation in patients with advanced solid tumours". ESMO Open. 3 (2): e000291. doi:10.1136/esmoopen-2017-000291.

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[1] "sapanisertib". NCI Drug Dictionary. National Cancer Institute. 2 February 2011. Retrieved 23 August 2019.

[2] ttps://searchusan.ama-assn.org/usan/documentDownload?uri=%2Funstructured%2Fbinary%2Fusan%2Fsapanisertib.pdf

[3] ttp://adisinsight.springer.com/drugs/800030541

[4] Moore, Kathleen N; Bauer, Todd M; Falchook, Gerald S; Chowdhury, Swapan; Patel, Chirag; Neuwirth, Rachel; Enke, Aaron; Zohren, Fabian; Patel, Manish R (February 2018). "Phase I study of the investigational oral mTORC1/2 inhibitor sapanisertib (TAK-228): tolerability and food effects of a milled formulation in patients with advanced solid tumours". ESMO Open. 3 (2): e000291. doi:10.1136/esmoopen-2017-000291.