Risovalisib CYH33|cas:1494684-28-4|西域试剂

Risovalisib CYH33,99.39%

产品编号：Bellancom-123938| CAS NO：1494684-28-4| 分子式：C₂₄H₂₉F₃N₈O₅S| 分子量：598.60

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-123938	￥5500.00	杭州北京（现货）
Bellancom-123938	￥9600.00	杭州北京（现货）
Bellancom-123938	￥15000.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

Risovalisib CYH33

产品介绍

Risovalisib (CYH33) 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。Risovalisib 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。Risovalisib 具有有效的抗实体瘤的活性。

生物活性

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

体外研究

Risovalisib (CYH33) 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) significantly arrests T47D and MCF7 cells in G1 phase in a concentration-dependent manner.
CYH33 (4-1000 nM; 1 hour) concurrently inhibits phosphorylation of ERK and Akt in both T47D and MCF7 cells.
CYH33 (0.11-1 μM; 24 hours) fails to induce apoptosis in MCF7 and MDA-MB-231 cells.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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
(In Vivo)

Risovalisib (CYH33) (2-20 mg/kg; oral; once a day for 21 days) potently restrains tumor growth in mice bearing human breast cancer cell xenografts.
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.
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-Pik3ca^H1047R;MMTV-Cre mice.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.