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CYH33 methanesulfonate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CYH33 methanesulfonate图片
CAS NO:1494684-33-1
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
CYH33 methanesulfonate 是一种具有口服活性的,高选择性PI3Kα抑制剂,对 α/β/δ/γ 亚型的IC50分别为 5.9 nM/598 nM/78.7 nM/225 nM。CYH33 methanesulfonate 抑制 Akt 和 ERK 的磷酸化,并显着诱导乳腺癌和非小细胞肺癌 (NSCLC) 细胞 G1 期阻滞。CYH33 methanesulfonate 具有有效的抗实体瘤的活性。
生物活性

CYH33 methanesulfonate is an orally active, highly selectivePI3Kαinhibitor withIC50s of 5.9 nM/598 nM/78.7 nM/225 nM against α/β/δ/γ isoform, respectively. CYH33 methanesulfonate inhibits phosphorylation ofAkt,ERKand induces significant G1 phase arrest in breastcancercells and non-small cell lungcancer(NSCLC) cells. CYH33 methanesulfonate 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)

体外研究
(In Vitro)

CYH33 methanesulfonate 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) methanesulfonate significantly arrests T47D and MCF7 cells in G1 phase in a concentration-dependent manner[2].
CYH33 (4-1000 nM; 1 hour) methanesulfonate concurrently inhibits phosphorylation of ERK and Akt in both T47D and MCF7 cells[2].
CYH33 (0.11-1 μM; 24 hours) methanesulfonate 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.
体内研究
(In Vivo)

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 (20 mg/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 (10 mg/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-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.
Clinical Trial
分子量

694.70

性状

Solid

Formula

C25H33F3N8O8S2

CAS 号

1494684-33-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)