PF-07104091 |
| Catalog No.GC62660 |
PF-07104091 es un inhibidor de CDK2/ciclina E1, un inhibidor selectivo del sitio de ATP que apunta al estado activado por la ciclina de la quinasa.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2460249-19-6
Sample solution is provided at 25 µL, 10mM.
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PF-07104091 is a CDK2/cyclin E1 inhibitor, a selective ATP-site inhibitor targeting the cyclin-bound activated state of the kinase [1]. PF-07104091(Example 13) inhibited CDK2/cyclin E1, GSK3β, CDK1/cyclin A2, CDK4/cyclin D1, CDK6/cyclin D3 and CDK9, with Kis of 1.16, 537.81, 110, 238, 465 and 117 nM, respectively. PF-07104091 has anti-tumor activity for cyclin E1-amplified cancers. [1].
PF-07104091 inhibited T47D and KPL1 cells with IC50s of 0.785 and 0.603 µM, respectively [2].
The combination of abemaciclib and PF-07104091decreased T47D and KPL1 cells survival compared to either single agent [2].
References:
[1]. Behenna, D. C.; Freeman-Cook, K. D.; Hoffman, R. L.; Nagata, A.; Ninkovic, S.; Sutton, S. C. Preparation of aminopyrazolylcyclopentyl carbamate derivatives for use as CDK2 inhibitors. WO 2020157652, 2020.
[2]. Gharbi S I, Pelletier L A, Espada A, et al. Crystal structure of active CDK4-cyclin D and mechanistic basis for abemaciclib efficacy[J]. npj Breast Cancer, 2022, 8(1): 126.
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