Pilaralisib

A class I PI3K inhibitor

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库存: 现货

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促销价

数量
5mg

￥1050.00

840.00

- +
10mg

￥1512.00

1210.00

- +
50mg

￥4000.00

3200.00

- +
100mg

￥0.00

0.00

- +
200mg

￥0.00

0.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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货号: ajce58076
CAS: 934526-89-3
别名: 2-氨基-N-[3-[N-[3-[(2-氯-5-甲氧基苯基)氨基]喹喔啉-2-基]氨基磺酰基]苯基]-2-甲基丙酰胺,XL-147; SAR245408
分子式: C25H25ClN6O4S
分子量: 541.02
纯度: >98%
溶解度: DMSO: ≥ 100 mg/mL (184.84 mM); Water: < 0.1 mg/mL (insoluble)
储存: Store at -20°C
库存: 现货

Background

XL147 is an inhibitor of class I PI3Ks (IC₅₀s = 0.039, 0.036, 0.023, and 0.383 ?M for p110α, -δ, -γ, and -β, respectively).¹ It is selective for class I PI3Ks over the class III PI3K vacuolar protein sorting 34 (Vps34; IC₅₀ = 6.974 ?M), as well as DNA protein kinase (DNA-PK) and mammalian target of rapamycin (mTOR) (IC₅₀s = 4.75 and >15 ?M, respectively). XL147 inhibits the proliferation of MCF-7 breast and PC3 prostate cancer cells (IC₅₀s = 9.669 and 16.492 ?M, respectively). It reduces tumor growth in a BT474 breast cancer mouse xenograft model when administered alone or in combination with trastuzumab or lapatinib .²

1.Foster, P., Yamaguchi, K., Hsu, P.P., et al.The selective PI3K inhibitor XL147 (SAR245408) inhibits tumor growth and survival and potentiates the activity of chemotherapeutic agents in preclinical tumor modelsMol. Cancer Ther.14(4)931-940(2015) 2.Chakrabarty, A., Sánchez, V., Kuba, M.G., et al.Feedback upregulation of HER3 (ErbB3) expression and activity attenuates antitumor effect of PI3K inhibitorsProc. Natl. Acad. Sci. USA109(8)2718-2723(2012)