CYH33 methanesulfonate - CAS:1494684-33-1

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CYH33 methanesulfonate

目录号 : KM10331 CAS No. : 1494684-33-1

Data Sheet 产品使用指南

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。

规格	价格	是否有货	数量
5mg		In-stock
10mg		In-stock

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生物活性

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.

体外研究

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

Cell Cycle Analysis

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

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

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.
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.
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-Pik3ca;MMTV-Cre mice.

Animal Model:	SCID mice aged 4-6 weeks bearing human breast cancer T47D xenografts
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.

分子式

C₂₅H₃₃F₃N₈O₈S₂

分子量

694.70

CAS号

1494684-33-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

Data Sheet

产品使用指南

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

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