Adavosertib

Adavosertib
Names
	Preferred IUPAC name 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
	Other names AZD1775; MK-1775
Identifiers
CAS Number	955365-80-7;
3D model (JSmol)	Interactive image;
ChEBI	CHEBI:91414;
ChEMBL	ChEMBL1976040;
ChemSpider	24808590;
ECHA InfoCard	100.205.373
IUPHAR/BPS	7702;
KEGG	D11361;
PubChem CID	24856436;
UNII	K2T6HJX3I3;
CompTox Dashboard (EPA)	DTXSID30241868 ;
	InChI InChI=1S/C27H32N8O2/c1-5-13-34-25(36)21-18-28-26(29-19-9-11-20(12-10-19)33-16-14-32(4)15-17-33)31-24(21)35(34)23-8-6-7-22(30-23)27(2,3)37/h5-12,18,37H,1,13-17H2,2-4H3,(H,28,29,31) Key: BKWJAKQVGHWELA-UHFFFAOYSA-N;
	SMILES CN1CCN(CC1)c2ccc(Nc3ncc4C(=O)N(CC=C)N(c5cccc(n5)C(C)(C)O)c4n3)cc2;
Properties
Chemical formula	C27H32N8O2
Molar mass	500.607 g·mol−1
	Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). Infobox references

Adavosertib (development codes AZD1775, MK-1775) is an experimental anti-cancer drug candidate. It is a small molecule inhibitor of the tyrosine kinase WEE1 with potential antineoplastic sensitizing activity.^[1] It is being developed by AstraZeneca.^[2] It is being investigated as a treatment for pancreatic cancer with a phase 1 trial (University of Michigan researchers are as of 2019 planning a phase 2 study.^[3]), and ovarian cancer, in combination with another anti-cancer drug, gemcitabine, as a phase 2 trial.^[4]^[5]^[6]

References

^ "NCI Drug Dictionary". National Cancer Institute. 2 February 2011. Retrieved 17 August 2019.
^ "AZD1775 | AstraZeneca Open Innovation". openinnovation.astrazeneca.com. Archived from the original on 17 August 2019. Retrieved 17 August 2019.
^ "AstraZeneca drug heads to phase 2 in pancreatic cancer after small trial extends survival". FierceBiotech. Retrieved 17 August 2019.
^ Lheureux S, Cristea MC, Bruce JP, Garg S, Cabanero M, Mantia-Smaldone G, Olawaiye AB, Ellard SL, Weberpals JI, Wahner Hendrickson AE, Fleming GF, Welch S, Dhani NC, Stockley T, Rath P (2021-01-23). "Adavosertib plus gemcitabine for platinum-resistant or platinum-refractory recurrent ovarian cancer: a double-blind, randomised, placebo-controlled, phase 2 trial". Lancet. 397 (10271): 281–292. doi:10.1016/S0140-6736(20)32554-X. ISSN 1474-547X. PMC 10792546. PMID 33485453. S2CID 231667519.
^ "Early Activity in Pancreatic Cancer With New Drug". www.medpagetoday.com. 16 August 2019. Retrieved 17 August 2019.
^ Cuneo KC, Morgan MA, Sahai V, Schipper MJ, Parsels LA, Parsels JD, et al. (October 2019). "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. 37 (29): 2643–2650. doi:10.1200/JCO.19.00730. PMC 7006846. PMID 31398082.

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[1] "NCI Drug Dictionary". National Cancer Institute. 2 February 2011. Retrieved 17 August 2019.

[2] "AZD1775 | AstraZeneca Open Innovation". openinnovation.astrazeneca.com. Archived from the original on 17 August 2019. Retrieved 17 August 2019.

[3] "AstraZeneca drug heads to phase 2 in pancreatic cancer after small trial extends survival". FierceBiotech. Retrieved 17 August 2019.

[4] Lheureux S, Cristea MC, Bruce JP, Garg S, Cabanero M, Mantia-Smaldone G, Olawaiye AB, Ellard SL, Weberpals JI, Wahner Hendrickson AE, Fleming GF, Welch S, Dhani NC, Stockley T, Rath P (2021-01-23). "Adavosertib plus gemcitabine for platinum-resistant or platinum-refractory recurrent ovarian cancer: a double-blind, randomised, placebo-controlled, phase 2 trial". Lancet. 397 (10271): 281–292. doi:10.1016/S0140-6736(20)32554-X. ISSN 1474-547X. PMC 10792546. PMID 33485453. S2CID 231667519.

[5] "Early Activity in Pancreatic Cancer With New Drug". www.medpagetoday.com. 16 August 2019. Retrieved 17 August 2019.

[6] Cuneo KC, Morgan MA, Sahai V, Schipper MJ, Parsels LA, Parsels JD, et al. (October 2019). "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. 37 (29): 2643–2650. doi:10.1200/JCO.19.00730. PMC 7006846. PMID 31398082.

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