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Afuresertib

编号: 25111
Cas号: 1047644-62-1
纯度: 98% Min.

Afuresertib, also known as GSK-2110183 or GSK-2110183C, is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. Afuresertib binds to and inhibits the activity of Akt, which may result in inhibition of the PI3K/Akt signaling pathway and tumor cell proliferation and the induction of tumor cell apoptosis. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis

仅供研究使用。 我们不向患者出售。

化学信息

名称Afuresertib
Iupac 化学名称2-Thiophenecarboxamide, N-((1S)-2-amino-1-((3-fluorophenyl)methyl)ethyl)-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-
同义词GSK2110183; GSK 2110183; GSK-2110183; GSK2110183C; GSK 2110183C; GSK2110183C; Afuresertib free base;
英文同义词GSK2110183; GSK 2110183; GSK-2110183; GSK2110183C; GSK 2110183C; GSK2110183C; Afuresertib free base;
分子式C18H17Cl2FN4OS
分子量427.32
SmileO=C(C1=CC(C2=C(Cl)C=NN2C)=C(Cl)S1)N[C@@H](CC3=CC=CC(F)=C3)CN
InChiKeyAFJRDFWMXUECEW-LBPRGKRZSA-N
InChiInChI=1S/C18H17Cl2FN4OS/c1-25-16(14(19)9-23-25)13-7-15(27-17(13)20)18(26)24-12(8-22)6-10-3-2-4-11(21)5-10/h2-5,7,9,12H,6,8,22H2,1H3,(H,24,26)/t12-/m0/s1
Cas号1047644-62-1
相关CAS号

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包装价格库存纯度备货期
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Request Bulk Quote Download MSDS 电话 : +86-177 0271 9238   Email : sales@sun-shinechem.com
外观性状类白色固体
纯度98% Min.
存储 0-4℃,可保存几天到几周;-20℃,可保存 几个月。
可溶性溶于DMSO等有机溶剂
处理方式
运输条件可以在室温下进行运输。
海关编码
Coming soon.
Targets
Mechanism
Cell study
Animal study
Clinical study

1: Uko NE, Güner OF, Matesic DF, Bowen JP. Akt Pathway Inhibitors. Curr Top Med Chem. 2020;20(10):883-900. doi: 10.2174/1568026620666200224101808. PMID: 32091335.


2: Min B, Wang Y, Liang F, Wang CX, Wang F, Yang Z. The Protective Mechanism of Afuresertib against Esophageal Cancer. Dis Markers. 2022 Jul 14;2022:1832241. doi: 10.1155/2022/1832241. PMID: 35872696; PMCID: PMC9303141.


3: Cho H, Abshire ET, Popp MW, Pröschel C, Schwartz JL, Yeo GW, Maquat LE. AKT constitutes a signal-promoted alternative exon-junction complex that regulates nonsense-mediated mRNA decay. Mol Cell. 2022 Aug 4;82(15):2779-2796.e10. doi: 10.1016/j.molcel.2022.05.013. Epub 2022 Jun 7. PMID: 35675814; PMCID: PMC9357146.


4: Zhou H, Ning Y, Zeng G, Zhou C, Ding X. Curcumin promotes cell cycle arrest and apoptosis of acute myeloid leukemia cells by inactivating AKT. Oncol Rep. 2021 Apr;45(4):11. doi: 10.3892/or.2021.7962. Epub 2021 Mar 2. PMID: 33649826; PMCID: PMC7877002.


5: Wu JH, Limmer AL, Narayanan D, Doan HQ, Simonette RA, Rady PL, Tyring SK. The novel AKT inhibitor afuresertib suppresses human Merkel cell carcinoma MKL-1 cell growth. Clin Exp Dermatol. 2021 Dec;46(8):1551-1554. doi: 10.1111/ced.14798. Epub 2021 Aug 26. PMID: 34115902.


6: Yamaji M, Ota A, Wahiduzzaman M, Karnan S, Hyodo T, Konishi H, Tsuzuki S, Hosokawa Y, Haniuda M. Novel ATP-competitive Akt inhibitor afuresertib suppresses the proliferation of malignant pleural mesothelioma cells. Cancer Med. 2017 Nov;6(11):2646-2659. doi: 10.1002/cam4.1179. Epub 2017 Sep 27. PMID: 28960945; PMCID: PMC5673922.


7: Blagden SP, Hamilton AL, Mileshkin L, Wong S, Michael A, Hall M, Goh JC, Lisyanskaya AS, DeSilvio M, Frangou E, Stronach EA, Gopalakrishna P, Meniawy TM, Gabra H. Phase IB Dose Escalation and Expansion Study of AKT Inhibitor Afuresertib with Carboplatin and Paclitaxel in Recurrent Platinum-resistant Ovarian Cancer. Clin Cancer Res. 2019 Mar 1;25(5):1472-1478. doi: 10.1158/1078-0432.CCR-18-2277. Epub 2018 Dec 18. PMID: 30563934.


8: Arceci RJ, Allen CE, Dunkel IJ, Jacobsen E, Whitlock J, Vassallo R, Morris SR, Portnoy A, Reedy BA, Smith DA, Noble R, Murnane A, Cornfeld M, Rodriguez- Galindo C, Heaney ML, McClain K, Vaiselbuh S. A phase IIa study of afuresertib, an oral pan-AKT inhibitor, in patients with Langerhans cell histiocytosis. Pediatr Blood Cancer. 2017 May;64(5). doi: 10.1002/pbc.26325. Epub 2016 Nov 2. PMID: 27804235.


9: Spencer A, Yoon SS, Harrison SJ, Morris SR, Smith DA, Brigandi RA, Gauvin J, Kumar R, Opalinska JB, Chen C. The novel AKT inhibitor afuresertib shows favorable safety, pharmacokinetics, and clinical activity in multiple myeloma. Blood. 2014 Oct 2;124(14):2190-5. doi: 10.1182/blood-2014-03-559963. Epub 2014 Jul 29. PMID: 25075128; PMCID: PMC4229853.


10: Chen CI, Paul H, Le LW, Wei EN, Snitzler S, Wang T, Levina O, Kakar S, Lau A, Queau M, Johnston JB, Smith DA, Trudel S. A phase 2 study of ofatumumab (Arzerra®) in combination with a pan-AKT inhibitor (afuresertib) in previously treated patients with chronic lymphocytic leukemia (CLL). Leuk Lymphoma. 2019 Jan;60(1):92-100. doi: 10.1080/10428194.2018.1468892. Epub 2018 Jun 19. PMID: 29916761.


11: Tolcher AW, Patnaik A, Papadopoulos KP, Rasco DW, Becerra CR, Allred AJ, Orford K, Aktan G, Ferron-Brady G, Ibrahim N, Gauvin J, Motwani M, Cornfeld M. Phase I study of the MEK inhibitor trametinib in combination with the AKT inhibitor afuresertib in patients with solid tumors and multiple myeloma. Cancer Chemother Pharmacol. 2015 Jan;75(1):183-9. doi: 10.1007/s00280-014-2615-5. Epub 2014 Nov 25. PMID: 25417902.


12: Naymagon L, Abdul-Hay M. Novel agents in the treatment of multiple myeloma: a review about the future. J Hematol Oncol. 2016 Jun 30;9(1):52. doi: 10.1186/s13045-016-0282-1. PMID: 27363832; PMCID: PMC4929712.


13: Kong W, Zhu L, Li T, Chen J, Fan B, Ji W, Zhang C, Cai X, Hu C, Sun X, Cao P. Azeliragon inhibits PAK1 and enhances the therapeutic efficacy of AKT inhibitors in pancreatic cancer. Eur J Pharmacol. 2023 Jun 5;948:175703. doi: 10.1016/j.ejphar.2023.175703. Epub 2023 Apr 5. PMID: 37028543.


14: Wang J, Xu X, Wang T, Guo Q, Dai X, Guo H, Zhang W, Cheng S, Chen X, Ding L. Ceritinib increases sensitivity of AKT inhibitors to gastric cancer. Eur J Pharmacol. 2021 Apr 5;896:173879. doi: 10.1016/j.ejphar.2021.173879. Epub 2021 Jan 28. PMID: 33515539.


15: Wang B, Jiang L, Guo H, Sun Q, Wang Y, Xie E, Xia Q. Screening of PI3K-Akt- targeting Drugs for Silkworm against Bombyx mori Nucleopolyhedrovirus. Molecules. 2019 Apr 1;24(7):1260. doi: 10.3390/molecules24071260. PMID: 30939726; PMCID: PMC6480691.


16: Keane NA, Glavey SV, Krawczyk J, O'Dwyer M. AKT as a therapeutic target in multiple myeloma. Expert Opin Ther Targets. 2014 Aug;18(8):897-915. doi: 10.1517/14728222.2014.924507. Epub 2014 Jun 6. PMID: 24905897.


17: Chen R, Ning Y, Zeng G, Zhou H, Zhou L, Xiao P, Li Z, Zhou J. The miR-193a-5p/NCX2/AKT axis promotes invasion and metastasis of osteosarcoma. J Cancer. 2021 Aug 8;12(19):5903-5913. doi: 10.7150/jca.60969. PMID: 34476004; PMCID: PMC8408106.


18: Karnan S, Hanamura I, Ota A, Takasugi S, Nakamura A, Takahashi M, Uchino K, Murakami S, Wahiduzzaman M, Quang Vu L, Rahman ML, Hasan MN, Hyodo T, Konishi H, Tsuzuki S, Yoshikawa K, Suzuki S, Ueda R, Ejiri M, Hosokawa Y, Takami A. CD52 is a novel target for the treatment of FLT3-ITD-mutated myeloid leukemia. Cell Death Discov. 2021 May 25;7(1):121. doi: 10.1038/s41420-021-00446-8. PMID: 34035227; PMCID: PMC8149417.


19: Wiechmann S, Ruprecht B, Siekmann T, Zheng R, Frejno M, Kunold E, Bajaj T, Zolg DP, Sieber SA, Gassen NC, Kuster B. Chemical Phosphoproteomics Sheds New Light on the Targets and Modes of Action of AKT Inhibitors. ACS Chem Biol. 2021 Apr 16;16(4):631-641. doi: 10.1021/acschembio.0c00872. Epub 2021 Mar 23. PMID: 33755436.


20: Ni H, Shirazi F, Baladandayuthapani V, Lin H, Kuiatse I, Wang H, Jones RJ, Berkova Z, Hitoshi Y, Ansell SM, Treon SP, Thomas SK, Lee HC, Wang Z, Davis RE, Orlowski RZ. Targeting Myddosome Signaling in Waldenström's Macroglobulinemia with the Interleukin-1 Receptor-Associated Kinase 1/4 Inhibitor R191. Clin Cancer Res. 2018 Dec 15;24(24):6408-6420. doi: 10.1158/1078-0432.CCR-17-3265. Epub 2018 Aug 20. PMID: 30126942; PMCID: PMC6295253.

化学结构

25111 - Afuresertib | CAS 1047644-62-1

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