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Risovalisib
$550 – $1,500
Products Details
Product Description
– Risovalisib (CYH33) is an orally active, highly selective PI3Kα inhibitor with IC50s of 5.9 nM/598 nM/78.7 nM/225 nM against α/β/δ/γ isoform, respectively. Risovalisib inhibits phosphorylation of Akt, ERK and induces significant G1 phase arrest in breast cancer cells and non-small cell lung cancer (NSCLC) cells. Risovalisib has potent activity against solid tumors[1][2][3].
Web ID
– HY-123938
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C24H29F3N8O5S
References
– [1]Haoyue Xiang, et al. Abstract LB-268: Discovery of clinical candidate methyl (5-(6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinopyrrolo[2,1-f][1,2,4]triazin-2-yl)-4-(trifluoromethyl)pyridin-2-yl)carbamate (CYH33) : A highly potent and selective PI3K alpha inhibitor for the treatment of advanced solid tumors. AACR Annual Meeting 2018; April 14-18, 2018|[2]Xue-Ling Liu, et al. Decrease in Phosphorylated ERK Indicates the Therapeutic Efficacy of a Clinical PI3Kα-selective Inhibitor CYH33 in Breast Cancer. Cancer Lett. 2018 Oct 1;433:273-282.|[3]Yuxiang Wang, et al. Simultaneous inhibition of PI3Kα and CDK4/6 synergistically suppresses KRAS-mutated non-small cell lung cancer. Cancer Biol Med. 2019 Feb;16(1):66-83.
CAS Number
– 1494684-28-4
Molecular Weight
– 598.60
Compound Purity
– 99.39
SMILES
– O=C(OC)NC1=NC=C(C(N=C2N3CCOCC3)=NN4C2=CC(CN5CCN(S(=O)(C)=O)CC5)=C4)C(C(F)(F)F)=C1
Clinical Information
– Phase 2
Research Area
– Cancer
Solubility
– DMSO : 50 mg/mL (ultrasonic)
Target
– PI3K
Isoform
– PI3Kα;PI3Kβ;PI3Kγ;PI3Kδ
Pathway
– PI3K/Akt/mTOR
Product type
– Reference compound
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