Narazaciclib,1357470-29-1

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Narazaciclib

CAS No. : 1357470-29-1

MCE 国际站：Narazaciclib

产品活性：Narazaciclib (ON123300) 是一种强效的，可透过血脑屏障的多激酶抑制剂，可抑制 CDK4 (IC₅₀=3.9 nM），Ark5 (IC₅₀=5 nM)，PDGFRβ (IC₅₀=26 nM)，FGFR1 (IC₅₀=26 nM)，RET (IC₅₀=9.2 nM) 和 FYN (IC₅₀=11 nM)。Narazaciclib 在脑肿瘤中抑制 Akt 磷酸化及激活 Erk。Narazaciclib 抑制 CDK6，IC₅₀ 为 9.82 nM。

研究领域：Cell Cycle/DNA Damage  |  PI3K/Akt/mTOR  |  Epigenetics  |  Protein Tyrosine Kinase/RTK

作用靶点：CDK  |  AMPK  |  PDGFR

In Vitro: Narazaciclib (ON123300) inhibits U87 glioma cell proliferation with an IC₅₀ of 3.4±0.1 μM.?Narazaciclib (1 and 10 μM) inhibits cell proliferation in a panel of 11 glioma models including a patient-derived model (GBM10).
?Narazaciclib (6.3 μM; 1 h) reduces phosphorylation of Akt and its downstream signaling components, P70S6K, 40S rpS6 and Rb S780, yet ON123300 induces Erk activation in U87 cells; both in a dose- and time-dependent manner.?ON123300 inhibits PI3Kδ with the IC₅₀ of 144nM.

In Vivo: Narazaciclib (ON123300) decreases p-Akt expression and increases p-Erk activity in brain tumors upon administration at both IV doses of 5 mg/kg and 25 mg/kg in U87 brain tumor-bearing mouse. The half-life (T_1/2) is 1.5 h for 5 mg/kg and 25 mg/kg in plasma.

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