Prexasertib

Prexasertib
Clinical data
Pregnancy; category	IV;
ATC code	none;
Identifiers
	IUPAC name 5-((5-(2-(3-Aminopropoxy)-6-methoxyphenyl)-1H-pyrazol-3-yl)amino)-2-pyrazinecarbonitrile;
CAS Number	1234015-52-1 ;
ChemSpider	32738771;
UNII	820NH671E6;
KEGG	D11206;
CompTox Dashboard (EPA)	DTXSID301031326 ;
Chemical and physical data
Formula	C18H19N7O2
Molar mass	365.397 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C1=C(C(=C(C=C1)OC)C1=CC(=NN1)NC1=NC=C(N=C1)C#N)OCCCN;
	InChI InChI=1S/C18H19N7O2/c1-26-14-4-2-5-15(27-7-3-6-19)18(14)13-8-16(25-24-13)23-17-11-21-12(9-20)10-22-17/h2,4-5,8,10-11H,3,6-7,19H2,1H3,(H2,22,23,24,25); Key:DOTGPNHGTYJDEP-UHFFFAOYSA-N;

Prexasertib (LY2606368) is a small molecule checkpoint kinase inhibitor, mainly active against CHEK1, with minor activity against CHEK2. This causes induction of DNA double-strand breaks resulting in apoptosis. It was developed by Eli Lilly but the company announced in 2019 it was dropping prexasertib from active development,^[1] although clinical trials continue. Research continues into the efficacy of prexasertib in treatment of acute myeloid leukemia, myelodysplastic syndrome, rhabdomyosarcoma, and medulloblastoma.^[2]

References

^ Al Idrus A (30 April 2019). "Lilly dumps phase 2 cancer drugs that survived previous cull". Fierce Biotech.
^ "Clinical Trials Using Prexasertib". National Cancer Institute, National Institutes of Health, U.S. Department of Health and Human Services.

[1] Al Idrus A (30 April 2019). "Lilly dumps phase 2 cancer drugs that survived previous cull". Fierce Biotech.

[2] "Clinical Trials Using Prexasertib". National Cancer Institute, National Institutes of Health, U.S. Department of Health and Human Services.

[1]

[2]

Clinical data

Pregnancy category	IV
ATC code	none
Identifiers
IUPAC name 5-((5-(2-(3-Aminopropoxy)-6-methoxyphenyl)-1H-pyrazol-3-yl)amino)-2-pyrazinecarbonitrile
CAS Number	1234015-52-1^Y
ChemSpider	32738771
UNII	820NH671E6
KEGG	D11206
CompTox Dashboard (EPA)	DTXSID301031326
Chemical and physical data
Formula	C₁₈H₁₉N₇O₂
Molar mass	365.397 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES C1=C(C(=C(C=C1)OC)C1=CC(=NN1)NC1=NC=C(N=C1)C#N)OCCCN
InChI InChI=1S/C18H19N7O2/c1-26-14-4-2-5-15(27-7-3-6-19)18(14)13-8-16(25-24-13)23-17-11-21-12(9-20)10-22-17/h2,4-5,8,10-11H,3,6-7,19H2,1H3,(H2,22,23,24,25) Key:DOTGPNHGTYJDEP-UHFFFAOYSA-N