1. PI3K/Akt/mTOR
  2. PI3K
  3. CYH33

CYH33 

Cat. No.: HY-123938
Handling Instructions

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. CYH33 inhibits phosphorylation of Akt, ERK and induces significant G1 phase arrest in breast cancer cells and non-small cell lung cancer (NSCLC) cells. CYH33 has potent activity against solid tumors.

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CYH33 Chemical Structure

CYH33 Chemical Structure

CAS No. : 1494684-28-4

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Description

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. CYH33 inhibits phosphorylation of Akt, ERK and induces significant G1 phase arrest in breast cancer cells and non-small cell lung cancer (NSCLC) cells. CYH33 has potent activity against solid tumors[1][2][3].

IC50 & Target[1]

PI3Kα

5.9 nM (IC50)

PI3Kβ

598 nM (IC50)

PI3Kδ

78.7 nM (IC50)

PI3Kγ

225 nM (IC50)

In Vitro

CYH33 inhibits cell proliferation with IC50s below 1 μM in 56% (18/32) of the breast cancer cell lines[2].
CYH33 (0.012-1 μM; for 24 hours) significantly arrests T47D and MCF7 cells in G1 phase in a concentration-dependent manner[2].
CYH33 (4-1000 nM; 1 hour) concurrently inhibits phosphorylation of ERK and Akt in both T47D and MCF7 cells[2].
CYH33 (0.11-1 μM; 24 hours) fails to induce apoptosis in MCF7 and MDA-MB-231 cells[2].

Cell Cycle Analysis[2]

Cell Line: Sensitive T47D, MCF7 and resistant MDA-MB-231 cells
Concentration: 0.012, 0.037, 0.11, 0.33, 1 μM
Incubation Time: For 24 hours
Result: Arrested T47D and MCF7 cells in G1 phase in a concentration-dependent manner, accompanied with concomitant reduced cell population in S phase.
Had little effect on cell cycle distribution in resistant MDA-MB-231 cells.

Western Blot Analysis[2]

Cell Line: Sensitive T47D, MCF7 and resistant MDA-MB-231 cells
Concentration: 4, 12, 37, 111, 333, 1000 nM
Incubation Time: 1 hour
Result: Concurrently inhibited phosphorylation of ERK and Akt in both T47D and MCF7 cells, whereas it had little effect on phosphorylated ERK (pERK) in MDA-MB-231 cells up to 1 μM.
In Vivo

CYH33 (2-20 mg/kg; oral; once a day for 21 days) potently restrains tumor growth in mice bearing human breast cancer cell xenografts[2].
Single administration of CYH33 (20 mg/kg; oral) significantly down-regulates the level of phosphorylated Akt in tumor tissues, demonstrating the suppression of PI3K signaling in nude mice[2].
CYH33 (10 mg/kg; oral; once a day for 18-d or 20-d respectively) delays the restoration of blood glucose and area under the curve (AUC) of blood glucose increased upon CYH33 treatment in T47D xenografts and R26-Pik3caH1047R;MMTV-Cre mice[2].

Animal Model: SCID mice aged 4-6 weeks bearing human breast cancer T47D xenografts[2]
Dosage: 2, 5, 10, 20 mg/kg
Administration: Oral; once a day for 21 days
Result: Displayed marginal inhibitory effect on the tumor growth at lower doses (2 and 5 mg/kg) and significantly attenuated tumor growth at the dose of 10 or 20 mg/kg, yielding T/C values of 58.36% and 49.42% respectively.
Molecular Weight

598.60

Formula

C₂₄H₂₉F₃N₈O₅S

CAS No.

1494684-28-4

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

CYH33CYH 33CYH-33PI3KPhosphoinositide 3-kinaseorallyphosphorylationAktERKproliferationbreastcancerT47DMCF7G1phaseMDA-MB-231Inhibitorinhibitorinhibit

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