QR-6401 | CDK2 inhibitor | Probechem Biochemicals

Chemical Structure : QR-6401

QR-6401 (QR6401)

Catalog No.: PC-20284Not For Human Use, Lab Use Only.

QR-6401 (QR6401) is a highly potent, selective, oral macrocyclic CDK2 inhibitor.

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Biological Activity

QR-6401 (QR6401) is a highly potent, selective, oral macrocyclic CDK2 inhibitor with IC50 of 0.37 nM (CDK2/Cyclin E1).
QR-6401 exhibits good selectivity against other closely related kinases, such as CDK1, CDK4, CDK6, CDK9 and GSK3β.
QR-6401 demonstrates good intrinsic metabolic stability and acceptable plasma protein binding in different species.
QR-6401 ( twice daily through oral gavage at 50 mg/kg for 28 days) caused significant tumor growth inhibition (TGI% = 78%) in OVCAR3 ovarian cancer xenograft model, produced robust suppression of Rb phosphorylation

Physicochemical Properties

M.Wt	369.43
Formula	C19H23N5O3
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(11S,13R,71R,73S,Z)-21H-6,10-dioxa-3,8-diaza-4(2,6)-pyridina-2(5,3)-pyrazola-1(1,3)-cyclopentana-7(1,3)-cyclobutanacyclodecaphan-9-one

References

1. Yang Yu, et al. ACS Med Chem Lett. 2023 Feb 8;14(3):297-304.

QR-6401 (QR6401)

Biological Activity

Physicochemical Properties

References

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