阿达色替

阿达色替
	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
别名	AZD1775; MK-1775
识别
CAS号	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配体	7702
性质
化学式	C27H32N8O2
摩尔质量	500.6 g·mol−1
	若非注明，所有数据均出自标准状态（25 ℃，100 kPa）下。

阿达色替（INN：adavosertib；开发代码：AZD1775、MK-1775），或译阿达替布，是一种实验性抗癌候选药物。它是酪氨酸激酶WEE1的小分子抑制剂，具有潜在的抗肿瘤致敏活性。^[1]它是由阿斯利康开发的。^[2]目前正在对它作为胰腺癌的治疗方法进行I期试验（截至2019年密歇根大学的研究人员计划进行II期研究）^[3]，以及与另一种抗癌药物吉西他滨联合用于卵巢癌的II期试验。^[4]^[5]^[6]

参考资料

^ NCI Drug Dictionary. National Cancer Institute. 2 February 2011 [17 August 2019]. （原始内容存档于2023-03-08）（英语）.
^ AZD1775 | AstraZeneca Open Innovation. openinnovation.astrazeneca.com. [17 August 2019]. （原始内容存档于17 August 2019）（英语）.
^ AstraZeneca drug heads to phase 2 in pancreatic cancer after small trial extends survival. FierceBiotech. [17 August 2019]. （原始内容存档于2023-05-30）（英语）.
^ 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]. （原始内容存档于2023-05-29）（英语）.
^ 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]. （原始内容存档于2023-03-08）（英语）.

[2] AZD1775 | AstraZeneca Open Innovation. openinnovation.astrazeneca.com. [17 August 2019]. （原始内容存档于17 August 2019）（英语）.

[3] AstraZeneca drug heads to phase 2 in pancreatic cancer after small trial extends survival. FierceBiotech. [17 August 2019]. （原始内容存档于2023-05-30）（英语）.

[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]. （原始内容存档于2023-05-29）（英语）.

[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.

[1]

[2]

[3]

[4]

[5]

[6]