2. PI3K/Akt/mTOR
  3. PI3K
  4. Risovalisib

Risovalisib  (Synonyms: CYH33)

目录号: HY-123938 纯度: 99.39%
COA 产品使用指南

摩尔计算器

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。

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Risovalisib Chemical Structure

Risovalisib Chemical Structure

CAS No. : 1494684-28-4

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规格 价格 是否有货 数量
1 mg ￥5500
In-stock
5 mg ￥9600
In-stock
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50 mg   询价  

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Customer Review

Other Forms of Risovalisib:

Risovalisib 相关抗体

Top Publications Citing Use of Products

查看 PI3K 亚型特异性产品:

查看所有亚型
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[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)

Risovalisib (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].

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

Risovalisib 相关抗体:

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)

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[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].

MCE 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[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

598.60

Formula

C24H29F3N8O5S
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 50 mg/mL (83.53 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6706 mL 8.3528 mL 16.7056 mL
5 mM 0.3341 mL 1.6706 mL 3.3411 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

Risovalisib 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6706 mL 8.3528 mL 16.7056 mL 41.7641 mL
5 mM 0.3341 mL 1.6706 mL 3.3411 mL 8.3528 mL
10 mM 0.1671 mL 0.8353 mL 1.6706 mL 4.1764 mL
15 mM 0.1114 mL 0.5569 mL 1.1137 mL 2.7843 mL
20 mM 0.0835 mL 0.4176 mL 0.8353 mL 2.0882 mL
25 mM 0.0668 mL 0.3341 mL 0.6682 mL 1.6706 mL
30 mM 0.0557 mL 0.2784 mL 0.5569 mL 1.3921 mL
40 mM 0.0418 mL 0.2088 mL 0.4176 mL 1.0441 mL
50 mM 0.0334 mL 0.1671 mL 0.3341 mL 0.8353 mL
60 mM 0.0278 mL 0.1392 mL 0.2784 mL 0.6961 mL
80 mM 0.0209 mL 0.1044 mL 0.2088 mL 0.5221 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Risovalisib1494684-28-4CYH33CYH 33CYH-33PI3KPhosphoinositide 3-kinaseorallyphosphorylationAktERKproliferationbreastcancerT47DMCF7G1phaseMDA-MB-231Inhibitorinhibitorinhibit

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