| Bioactivity | Crozbaciclib fumarate is a CDK4/6 inhibitor with IC50s of 3 and 1 nM, respectively. |
| Target | IC50: 3 nM (CDK4), 1 nM (CDK6) |
| Invitro | Crozbaciclib fumarate 是一种有效的抗增殖剂，可将 U87MG 细胞系完全抑制在 G1 期（抗增殖试验中的 IC50=15.3 ± 2.9 nM）。 Crozbaciclib fumarate (13.72 nM; 24 h)显着增加 U87MG 细胞中 G1 期细胞的百分比[1]。 |
| In Vivo | Crozbaciclib fumarate (3.125-50 mg/kg) 在多形性胶质母细胞瘤原位异种移植小鼠模型中具有 62% 至 99% 的肿瘤生长抑制值。 而 Crozbaciclib fumarate 导致体重减轻不明显。 在 50 mg/kg[1] 的剂量下，Crozbaciclib fumarate 显着延长了 162% 的小鼠中载体处理动物的平均存活时间，显着延长了寿命。 |
| Name | Crozbaciclib fumarate |
| CAS | 2567494-39-5 |
| Formula | C32H34F2N6O4 |
| Molar Mass | 604.65 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Yin L, et al. A highly potent CDK4/6 inhibitor was rationally designed to overcome blood brain barrier in gliobastoma therapy. Eur J Med Chem. 2018 Jan 20;144:1-28. |