阿達色替

阿達色替
	IUPAC名; 1-[6-(2-Hydroxypropan-2-yl)pyridin-2-yl]-6-[4-(4-methylpiperazin-1-yl)anilino]-2-(prop-2-en-1-yl)-1,2-dihydro-3H-pyrazolo[3,4-d]pyrimidin-3-one
別名	AZD1775; MK-1775
識別
CAS號	955365-80-7
PubChem	24856436
ChemSpider	24808590
SMILES	CN1CCN(CC1)c2ccc(Nc3ncc4C(=O)N(CC=C)N(c5cccc(n5)C(C)(C)O)c4n3)cc2;
ChEBI	91414
KEGG	D11361
IUPHAR配體	7702
性質
化學式	C27H32N8O2
摩爾質量	500.6 g·mol−1
	若非註明，所有數據均出自標準狀態（25 ℃，100 kPa）下。

阿達色替（INN：adavosertib；開發代碼：AZD1775、MK-1775），或譯阿達替布，是一種實驗性抗癌候選藥物。它是酪氨酸激酶WEE1的小分子抑制劑，具有潛在的抗腫瘤致敏活性。^[1]它是由阿斯利康開發的。^[2]目前正在對它作為胰腺癌的治療方法進行I期試驗（截至2019年密歇根大學的研究人員計劃進行II期研究）^[3]，以及與另一種抗癌藥物吉西他濱聯合用於卵巢癌的II期試驗。^[4]^[5]^[6]

參考資料[編輯]

^ NCI Drug Dictionary. National Cancer Institute. 2 February 2011 [17 August 2019]. （原始內容存檔於2023-03-08）（英語）.
^ AZD1775 | AstraZeneca Open Innovation. openinnovation.astrazeneca.com. [17 August 2019]. （原始內容存檔於17 August 2019）（英語）.
^ AstraZeneca drug heads to phase 2 in pancreatic cancer after small trial extends survival. FierceBiotech. [17 August 2019]. （原始內容存檔於2023-05-30）（英語）.
^ Lheureux, Stephanie; Cristea, Mihaela C.; Bruce, Jeffrey P.; Garg, Swati; Cabanero, Michael; Mantia-Smaldone, Gina; Olawaiye, Alexander B.; Ellard, Susan L.; Weberpals, Johanne I.; Wahner Hendrickson, Andrea E.; Fleming, Gini F.; Welch, Stephen; Dhani, Neesha C.; Stockley, Tracy; Rath, Prisni. Adavosertib plus gemcitabine for platinum-resistant or platinum-refractory recurrent ovarian cancer: a double-blind, randomised, placebo-controlled, phase 2 trial. Lancet. 2021-01-23, 397 (10271): 281–292. ISSN 1474-547X. PMC 10792546 . PMID 33485453. S2CID 231667519. doi:10.1016/S0140-6736(20)32554-X .
^ Early Activity in Pancreatic Cancer With New Drug. www.medpagetoday.com. 16 August 2019 [17 August 2019]. （原始內容存檔於2023-05-29）（英語）.
^ Cuneo KC, Morgan MA, Sahai V, Schipper MJ, Parsels LA, Parsels JD, et al. Dose Escalation Trial of the Wee1 Inhibitor Adavosertib (AZD1775) in Combination With Gemcitabine and Radiation for Patients With Locally Advanced Pancreatic Cancer. Journal of Clinical Oncology. October 2019, 37 (29): 2643–2650. PMC 7006846 . PMID 31398082. doi:10.1200/JCO.19.00730.

[1] NCI Drug Dictionary. National Cancer Institute. 2 February 2011 [17 August 2019]. （原始內容存檔於2023-03-08）（英語）.

[2] AZD1775 | AstraZeneca Open Innovation. openinnovation.astrazeneca.com. [17 August 2019]. （原始內容存檔於17 August 2019）（英語）.

[3] AstraZeneca drug heads to phase 2 in pancreatic cancer after small trial extends survival. FierceBiotech. [17 August 2019]. （原始內容存檔於2023-05-30）（英語）.

[4] Lheureux, Stephanie; Cristea, Mihaela C.; Bruce, Jeffrey P.; Garg, Swati; Cabanero, Michael; Mantia-Smaldone, Gina; Olawaiye, Alexander B.; Ellard, Susan L.; Weberpals, Johanne I.; Wahner Hendrickson, Andrea E.; Fleming, Gini F.; Welch, Stephen; Dhani, Neesha C.; Stockley, Tracy; Rath, Prisni. Adavosertib plus gemcitabine for platinum-resistant or platinum-refractory recurrent ovarian cancer: a double-blind, randomised, placebo-controlled, phase 2 trial. Lancet. 2021-01-23, 397 (10271): 281–292. ISSN 1474-547X. PMC 10792546 . PMID 33485453. S2CID 231667519. doi:10.1016/S0140-6736(20)32554-X .

[5] Early Activity in Pancreatic Cancer With New Drug. www.medpagetoday.com. 16 August 2019 [17 August 2019]. （原始內容存檔於2023-05-29）（英語）.

[6] Cuneo KC, Morgan MA, Sahai V, Schipper MJ, Parsels LA, Parsels JD, et al. Dose Escalation Trial of the Wee1 Inhibitor Adavosertib (AZD1775) in Combination With Gemcitabine and Radiation for Patients With Locally Advanced Pancreatic Cancer. Journal of Clinical Oncology. October 2019, 37 (29): 2643–2650. PMC 7006846 . PMID 31398082. doi:10.1200/JCO.19.00730.

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