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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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PF-07224826 is a CDK2/4/6 inhibitor. |
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| Senexin B
Senexin B is a potent, orally active CDK8/19 inhibitor with Kd values of 140 nM and 80 nM for CDK8 and CDK19, respectively. |
| Q901
Q901 is a CDK7 inhibitor for tumor-related studies. |
| NUV-422
NUV-422 is a CDK2/4/6 inhibitor that can be used in studies related to malignant gliomas. |
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