CYH33 methanesulfonate Biochemical

CYH33 methanesulfonate

Cat. Num. AAA227756

• Purity: 98%
• Synonyms: CYH33 methanesulfonate; N/A; CYH33 methanesulfonate biochemical

• Purity/Purification: 98%

• CAS: 1494684-33-1
• Targets&IC50: PI3Kgamma:225 nM (IC50), PI3Kalpha:5.9 nM (IC50), PI3Kbeta:598 nM (IC50), PI3Kdelta:78.7 nM (IC50)
• Solubility: <1mg/ml refers to the product slightly soluble or insoluble
• In vitro: CYH33 (2-20 mg/kg; oral; once a day for 21 days) methanesulfonate potently restrains tumor growth in mice bearing human breast cancer cell xenografts[2]. Single administration of CYH33 (20mg/kg; oral) methanesulfonate significantly down-regulates the level of phosphorylated Akt in tumor tissues, demonstrating the suppression of PI3K signaling in nude mice[2]. CYH33 (10mg/kg; oral; once a day for 18-d or 20-d respectively) methanesulfonate delays the restoration of blood glucose and area under the curve (AUC) of blood glucose increased upon CYH33 treatment in T47D xenografts and R26-Pik3ca H1047R ;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 5mg/kg) and significantly attenuated tumor growth at the dose of 10 or 20mg/kg, yielding T/C values of 58.36% and 49.42% respectively.
• Preparation and Storage: Powder: -20 degree C for 3 years; In solvent: -80 degree C for 2 years

Structure

(PYBG-TMR, CAS 2067339-51-7)

Structure

(PYBG-TMR, CAS 2067339-51-7)

Related Product Information for CYH33 methanesulfonate biochemical

CYH33 methanesulfonate is an orally active, highly selective PI3Kalpha inhibitor with IC 50 s of 5.9 nM/598 nM/78.7 nM/225 nM against alpha/beta/delta/gamma 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.

References

1. Xinbo Song, et al. Terminal alkyne substituted O 6 -benzylguanine for versatile and effective syntheses of fluorescent labels to genetically encoded SNAP-tags. RSC Advances. 26 Feb 2015.