ChemicalBook >> CAS DataBase List >>Cyclobutanol, 3-amino-1-methyl-3-[4-(3-phenyl-5H-imidazo[1,2-c]pyrido[3,4-e][1,3]oxazin-2-yl)phenyl]-, hydrochloride (1:1), trans-

Cyclobutanol, 3-amino-1-methyl-3-[4-(3-phenyl-5H-imidazo[1,2-c]pyrido[3,4-e][1,3]oxazin-2-yl)phenyl]-, hydrochloride (1:1), trans-

CAS No.
2930090-28-9
Chemical Name:
Cyclobutanol, 3-amino-1-methyl-3-[4-(3-phenyl-5H-imidazo[1,2-c]pyrido[3,4-e][1,3]oxazin-2-yl)phenyl]-, hydrochloride (1:1), trans-
Synonyms
Cyclobutanol, 3-amino-1-methyl-3-[4-(3-phenyl-5H-imidazo[1,2-c]pyrido[3,4-e][1,3]oxazin-2-yl)phenyl]-, hydrochloride (1:1), trans-
CBNumber:
CB013626200
Molecular Formula:
C26H24N4O2.ClH
Molecular Weight:
460.96
MDL Number:
MOL File:
2930090-28-9.mol
Last updated:2025-04-18 09:51:25

Cyclobutanol, 3-amino-1-methyl-3-[4-(3-phenyl-5H-imidazo[1,2-c]pyrido[3,4-e][1,3]oxazin-2-yl)phenyl]-, hydrochloride (1:1), trans- Properties

form Solid
color White to yellow

Cyclobutanol, 3-amino-1-methyl-3-[4-(3-phenyl-5H-imidazo[1,2-c]pyrido[3,4-e][1,3]oxazin-2-yl)phenyl]-, hydrochloride (1:1), trans- Chemical Properties,Uses,Production

Uses

Pifusertib (TAS-117) hydrochloride is a potent, selective, orally active allosteric Akt inhibitor (with IC50s of 4.8, 1.6, and 44 nM for Akt1, 2, and 3, respectively). Pifusertib hydrochloride triggers anti-myeloma activities and enhances fatal endoplasmic reticulum (ER) stress induced by proteasome inhibition. Pifusertib hydrochloride induces apoptosis and autophagy[1].

in vivo

Pifusertib (12-16 mg/kg; p.o.; daily for 5 days a week, 21 days) inhibits tumor growth in murine xenograft models of human MM[1].
Pifusertib enhances bortezomib-induced MM cytotoxicity in vivo[1].

Animal Model:SCID mice (xenograft models bearing MM.1S cells)[1]
Dosage:12, 16 mg/kg
Administration:P.o.; daily for 5 days a week, 21 days
Result:Significantly reduced MM.1S tumor growth versus vehicle control.

IC 50

Akt1: 4.8 nM (IC50); Akt2: 1.6 nM (IC50); Akt3: 44 nM (IC50)

References

[1] Mimura N, et al. Selective and potent Akt inhibition triggers anti-myeloma activities and enhances fatal endoplasmic reticulum stress induced by proteasome inhibition. Cancer Res. 2014;74(16):4458-4469. DOI:10.1158/0008-5472.CAN-13-3652

Cyclobutanol, 3-amino-1-methyl-3-[4-(3-phenyl-5H-imidazo[1,2-c]pyrido[3,4-e][1,3]oxazin-2-yl)phenyl]-, hydrochloride (1:1), trans- Preparation Products And Raw materials

Raw materials

Preparation Products

Cyclobutanol, 3-amino-1-methyl-3-[4-(3-phenyl-5H-imidazo[1,2-c]pyrido[3,4-e][1,3]oxazin-2-yl)phenyl]-, hydrochloride (1:1), trans- Suppliers

Global( 2)Suppliers
Supplier Tel Email Country ProdList Advantage
Nantong QuanYi Biotechnology Co., Ltd 0513-66337626 18051384581 sales@chemhifuture.com China 5638 58
Guangzhou Yansai Biological Products Co., Ltd. 13710209565 CHINA 0 58
Cyclobutanol, 3-amino-1-methyl-3-[4-(3-phenyl-5H-imidazo[1,2-c]pyrido[3,4-e][1,3]oxazin-2-yl)phenyl]-, hydrochloride (1:1), trans- 2930090-28-9