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Abemaciclib (LY2835219) is a best-in-class, selective and effective dual inhibitor of CDK4 and CDK6, which inhibits CDK4/CDK6 activity with IC50 of 2 nM and 10 nM respectively. LY2835219 is an orally effective cyclin-dependent kinase (CDK) inhibitor that targets CDK4 (Cyclin D1) and CDK6 (cyclin D3) cell cycle pathways and has potential antitumor activity. LY2835219 specifically inhibits CDK4 and 6, thereby inhibiting the phosphorylation of retinoblastoma (Rb) protein in the early G1 phase. Abemaciclib (LY2835219) inhibits Rb phosphorylation and prevents CDK-mediated G1-S phase transition, resulting in cell cycle stagnation in G1 phase, inhibiting DNA synthesis, and inhibiting cancer cell growth.
Molecular Weight | 506.59 |
Formula | C27H32F2N8 |
CAS Number | 1231929-97-7 |
Solubility (25°C) | DMSO 3 mg/mL (ultrasonic and warming) |
Storage | 2-8°C, protect from light, sealed |
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(E/Z)-Zotiraciclib citrate
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Abemaciclib metabolites M2
Abemaciclib metabolite M2 (LSN2839567) is a metabolite of Abemaciclib, acts as a potent CDK4 and CDK6 inhibitor, with IC50 values of 1.2 and 1.3 nM, respectively. |
CDK9-IN-1
CDK9-IN-1 is a novel, selective CDK9 inhibitor, with an IC50 of 39 nM for CDK9/CycT1, it can be used for the research of HIV infection. |
XO44
XO44 (PF-6808472) is a broad-spectrum covalent kinase probe. |
ML 315
ML 315 is a selective dual inhibitor of CDK and DYRK with IC50s of 68 nM and 282 nM, respectively. |
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