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CYH33 (methanesulfonate)
$950 – $7,700
Products Details
Product Description
– CYH33 methanesulfonate 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. CYH33 methanesulfonate inhibits phosphorylation of Akt, ERK and induces significant G1 phase arrest in breast cancer cells and non-small cell lung cancer (NSCLC) cells. CYH33 methanesulfonate has potent activity against solid tumors[1][2][3].
Web ID
– HY-123938A
Storage Temperature
– 4°C (Powder, sealed storage, away from moisture)
Shipping
– Room Temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C25H33F3N8O8S2
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
– 1494684-33-1
Molecular Weight
– 694.70
Compound Purity
– 96.76
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.CS(=O)(O)=O
Clinical Information
– Phase 2
Research Area
– Cancer
Solubility
– 10 mM in DMSO
Target
– PI3K
Isoform
– PI3Kα;PI3Kβ;PI3Kγ;PI3Kδ
Pathway
– PI3K/Akt/mTOR
Product type
– Reference compound
Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.
