1820902-72-4
Chemical Structure
Bimiralisib hydrochloride
Synonym(s): PQR309 hydrochloride
- CAS. Nr.: 1820902-72-4
- Formula:C17H21ClF3N7O2
- Molecular Weight:447.84
IUPAC Name: 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine hydrochloride
InChIKey: VNBNQGZQKUMKAL-UHFFFAOYSA-N
SMILES: FC(F)(C1=CC(N)=NC=C1C2=NC(N3CCOCC3)=NC(N4CCOCC4)=N2)F.Cl
Biological Activity: Bimiralisib hydrochloride (PQR309 hydrochloride) is an orally active, blood-brain barrier-penetrant PI3K/mTOR inhibitor with in vitro antiproliferative activity and in vivo antitumor activity. Bimiralisib hydrochloride induces G1 cell cycle arrest, apoptosis and cell death in cancer cells, while inhibiting cancer cell proliferation, migration, invasion, colony formation and spheroid generation. Bimiralisib hydrochloride upregulates the expression of E2F4. The combination of Bimiralisib hydrochloride with venetoclax enhances therapeutic efficacy in acute myeloid leukemia models. Bimiralisib hydrochloride can be used in cancer-related research[1][2][3][4].
| Art. -Nr. | Produktname | Reinheit | Beschreibung | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
Bimiralisib hydrochloride | Bimiralisib hydrochloride (PQR309 hydrochloride) is an orally active, blood-brain barrier-penetrant PI3K/mTOR inhibitor with in vitro antiproliferative activity and in vivo antitumor activity. Bimiralisib hydrochloride induces G1 cell cycle arrest, apoptosis and cell death in cancer cells, while inhibiting cancer cell proliferation, migration, invasion, colony formation and spheroid generation. Bimiralisib hydrochloride upregulates the expression of E2F4. The combination of Bimiralisib hydrochloride with venetoclax enhances therapeutic efficacy in acute myeloid leukemia models. Bimiralisib hydrochloride can be used in cancer-related research. | |||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
References
- [1]. Wu X, et al. Recent Advances in Dual PI3K/mTOR Inhibitors for Tumour Treatment. Frontiers in pharmacology. 2022;13:875372.
- [2]. Seipel K, et al. Rationale for Combining the BCL2 Inhibitor Venetoclax with the PI3K Inhibitor Bimiralisib in the Treatment of IDH2- and FLT3-Mutated Acute Myeloid Leukemia. International journal of molecular sciences. 2022 Oct 20;23(20):12587. [Content Brief]
- [3]. Noh YJ, et al. Bimiralisib suppresses proliferation and migration of gastric cancer cells PI3K/mTOR pathway inhibition. The Korean journal of physiology & pharmacology : official journal of the Korean Physiological Society and the Korean Society of Pharmacology. 2026 Jul 08. [Content Brief]
- [4]. Beaufils F, et al. 5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology. J Med Chem. 2017 Sep 14;60(17):7524-7538.
