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CYH33 methanesulfonate

Catalog No. T38979 CAS 1494684-33-1

Synonyms: CYH33 methanesulfonate

CYH33 methanesulfonate is a highly selective and orally active inhibitor of PI3Kα, with IC50 values of 5.9 nM, 598 nM, 78.7 nM, and 225 nM against the α, β, δ, and γ isoforms, respectively. This compound effectively inhibits the phosphorylation of Akt and ERK, leading to a significant G1 phase arrest in breast cancer cells and non-small cell lung cancer (NSCLC) cells. Additionally, CYH33 methanesulfonate demonstrates potent activity against solid tumors.

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CYH33 methanesulfonate Chemical Structure

CYH33 methanesulfonate, CAS 1494684-33-1

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10 mg	Inquiry	$ 1,220.00

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Description	CYH33 methanesulfonate is a highly selective and orally active inhibitor of PI3Kα, with IC50 values of 5.9 nM, 598 nM, 78.7 nM, and 225 nM against the α, β, δ, and γ isoforms, respectively. This compound effectively inhibits the phosphorylation of Akt and ERK, leading to a significant G1 phase arrest in breast cancer cells and non-small cell lung cancer (NSCLC) cells. Additionally, CYH33 methanesulfonate demonstrates potent activity against solid tumors.
Targets&IC50	PI3Kγ:225 nM (IC50), PI3Kα:5.9 nM (IC50), PI3Kβ:598 nM (IC50), PI3Kδ:78.7 nM (IC50)
In vitro	CYH33 methanesulfonate demonstrates inhibitory effects on cell proliferation, showing IC50 values below 1μM in 56% (18/32) of breast cancer cell lines tested. In a concentration-dependent manner, CYH33 (0.012-1 μM; 24 hours) significantly arrests T47D and MCF7 cells in the G1 phase and concurrently diminishes the phosphorylation of ERK and Akt in these cells (4-1000 nM; 1 hour), indicating targeted action on key cell cycle and survival pathways. However, it does not induce apoptosis in MCF7 and MDA-MB-231 cells (0.11-1 μM; 24 hours). Cell cycle analysis further confirmed that CYH33 arrests sensitive T47D and MCF7 cells in the G1 phase in a concentration-dependent manner, reducing the S phase cell population, with minimal effects on the resistant MDA-MB-231 cell cycle distribution. Western blot analysis supports these findings, showing inhibited phosphorylation of ERK and Akt in sensitive cell lines without significant impact on phosphorylated ERK (pERK) in MDA-MB-231 cells up to 1μM.
In vivo	Administered orally at doses ranging from 2-20 mg/kg once daily for 21 days, CYH33 methanesulfonate effectively inhibits tumor growth in SCID mice implanted with human breast cancer T47D xenografts. At the highest dosage (20 mg/kg), it significantly reduces phosphorylated Akt levels in tumor tissues, indicating the suppression of the PI3K signaling pathway. Additionally, CYH33 methanesulfonate, at a dosage of 10 mg/kg given daily for 18 to 20 days, delays the recovery of blood glucose levels and increases the area under the curve (AUC) for blood glucose in T47D xenograft and R26-Pik3ca H1047R; MMTV-Cre mice models. The study shows a minimal inhibitory effect on tumor growth at lower doses (2 and 5 mg/kg), while doses of 10 or 20 mg/kg significantly reduce tumor growth, with T/C values of 58.36% and 49.42%, respectively.

Synonyms	CYH33 methanesulfonate
Molecular Weight	694.7
Formula	C25H33F3N8O8S2
CAS No.	1494684-33-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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.

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Keywords

CYH33 methanesulfonate 1494684-33-1 CYH-33 methanesulfonate inhibitor inhibit

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