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
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
Supplier | Tel | 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 |
Supplier | Advantage |
---|---|
Nantong QuanYi Biotechnology Co., Ltd | 58 |
Guangzhou Yansai Biological Products Co., Ltd. | 58 |