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上海源葉生物科技有限公司
主營產(chǎn)品： S30260異硫氰酸胍,30259鹽酸胍,嗜熱菌蛋白酶 |
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15921386130
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- 聯(lián)系人：
- 何小姐
- 電話：
- 86-021-61559134
- 手機(jī)：
- 15921386130
- 傳真：
- 86-021-55068248
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- 上海市松江區(qū)長塔路465號(hào)6幢
- 郵編：
- 200433
- 網(wǎng)址：
- www.shyuanye.com
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- 靶點(diǎn)： Apitolisib (GDC-0980; GNE 390; RG 7422) is a selective, potent, orally bioavailable Class I PI3 kinase and mTOR kinase (TORC1/2)
- 體外研究： Apitolisib (GDC-0980) is remarkably selective for several other members of the closely related PIKK family kinases: C2alpha IC50=1300 nM; C2beta IC50=7 94 nM; VPS34 IC50=2000 nM; PI4Kalpha >10 μM; PI4Kbeta >10 μM; DNA-PK Kiapp=623 nM, respectively. A recent study shows that Apitolisib (GDC-0980) reduces cancer cell viability by inhibiting cell-cycle procession and inducing apoptosis with most potency in prostate (IC50 < 200="" nm="" 50%),=""><500 nm="" 100%),="" breast="" (ic50=""><200 nm="" 37%,=""><500 nm="" 78%)="" and="" nsclc="" lines="" (ic50=""><200 nm="" 29%,=""><500 nm="" 88%)="" and="" less="" potency="" in="" pancreatic="" (ic50=""><200 nm="" 13%,=""><500 nm="" 67%)="" and="" melanoma="" cell="" lines="" (ic50=""><200 nm="" 0%,=""><500 nm="" 33%).="">
- 體內(nèi)研究： Apitolisib (GDC-0980) (1 mg/kg, p.o.) demonstrats significant efficacy in mouse xenografts and is currently in phase I clinical trials for cancer. Clearance and PPB are low, and Apitolisib (GDC-0980) shows dose-proportional exposure from 5 mg/kg dosed in PEG to 50 mg/kg dosed in suspension in MCT, a finding attributed partially to the compound’s good solubility. Apitolisib (GDC-0980) (5 mg/kg, p.o.) results in greater than 50% TGI in 15 of the 20 xenograft models. The difference in tumor response to Apitolisib (GDC-0980) treatment correlates with the duration of knockdown of pAkt/tAkt.
- 參考文獻(xiàn)：
[1]. Sutherlin DP, et al. Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer. J Med Chem, 2011, 54(21), 7579-7587.
[2]. Wallin JJ, et al. GDC-0980 is a novel class I PI3K/mTOR kinase inhibitor with robust activity in cancer models driven by the PI3K pathway. Mol Cancer Ther, 2011, 10(12), 2426-2436.
- 溶解度： soluble in DMSO
- 保存條件： -20℃
- 配置溶液濃度參考：
1mg 5mg 10mg 1 mM 2.006 ml 10.028 ml 20.056 ml 5 mM 0.401 ml 2.006 ml 4.011 ml 10 mM 0.201 ml 1.003 ml 2.006 ml 50 mM 0.04 ml 0.201 ml 0.401 ml
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