CH5132799

An inhibitor of class I PI3K isoforms

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库存: 现货

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5mg

￥1362.00

1090.00

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10mg

￥2387.00

1910.00

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50mg

￥5812.00

4650.00

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200mg

￥16462.00

13170.00

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货号: ajci7978
CAS: 1007207-67-1
别名: [5-[7-甲磺酰基-2-(吗啉-4-基)-6,7-二氢-5H-吡咯并[2,3-D]嘧啶-4-基]嘧啶-2-基]胺,CH5132799
分子式: C15H19N7O3S
分子量: 377.42
纯度: >98%
溶解度: DMSO: 12 mg/mL
储存: Store at -20°C
库存: 现货

Background

CH5132799 is an inhibitor of class I phosphatidylinositol 3-kinase (PI3K) with IC50 value of 14nM against PI3Kα [1].

CH5132799 shows inhibitory effect on class I PI3K with IC50 values of 0.014μM, 0.12μM, 0.5μM and 0.036μM against PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ, respectively. PI3Kα is especially sensitive to CH5132799. CH5132799 is a selective inhibitor. It shows less effect on class II PI3Ks, class III PI3K and mTOR. For other 26 protein kinases, CH5132799 nearly has no inhibition with IC50 value of > 10μM. CH5132799 is found to have potent antitumor activity. It exerts IC50 values of 0.2μM, 0.032μM, 0.056μM and 0.12μM in HCT116, KPL-4, T-47D and SK-OV-3 cell lines, respectively. Moreover, CH5132799 is oral available in animal models. Treatment of CH5132799 shows strong tumor regression at dose of 12.5 mg/kg in mice bearing human breast cancer xenografts [1].

参考文献:
[1] Ohwada J, Ebiike H, Kawada H, et al. Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799. Bioorganic & medicinal chemistry letters, 2011, 21(6): 1767-1772.

Protocol

Cell experiment:

The cell lines are added to the wells of 96-well plates containing 0.076 to 10,000 nM CH5132799 and incubated at 37°C. After 4 days of incubation, Cell Counting Kit-8 solution is added and, after incubation for several more hours, absorbance at 450 nm is measured with Microplate-Reader iMark. The antiproliferative activity is calculated. The IC50 values are calculated[1].

Animal experiment:

Mice[1] Female BALB-nu/nu mice (CAnN.Cg-Foxn1/CrlCrlj nu/nu) are used. A total of 4×106 to 1.2×107 cells are suspended in 100 to 200 μL serum-free culture medium and injected subcutaneously into the right flank of the mice. Tumor size is measured by using a gauge twice per week, and tumor volume (TV) is calculated. Once the tumors reach a volume of approximately 200 to 300 mm3, animals are randomized into groups (n=4 or 5 in each group) and treatment is initiated. CH5132799 and Everolimus are orally administered once a day and Trastuzumab is intravenously injected once a week.

参考文献:

[1]. Tanaka H, et al. The selective class I PI3K inhibitor CH5132799 targets human cancers harboring oncogenic PIK3CA mutations. Clin Cancer Res, 2011, 17(10), 3272-3281.
[2]. Ohwada J, et al. Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799. Bioorg Med Chem Leff, 2011, 21(6), 1767-1772.