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MedChemExpress - Model Narazaciclib -1357470-29-1

Narazaciclib (ON123300), a strong and brain-penetrant[1] multi-kinase inhibitor, inhibits CDK4 (IC50=3.9 nM), Ark5 (IC50=5 nM), PDGFRβ (IC50=26 nM), FGFR1 (IC50=26 nM), RET (IC50=9.2 nM), and FYN (IC50=11 nM). Single agent Narazaciclib causes a dose-dependent suppression of phosphorylation of Akt as well as activation of Erk in brain tumors[2]. Narazaciclib inhibits CDK6 with an IC50 of 9.82 nM[3].

Narazaciclib

MCE China：Narazaciclib

Brand：MedChemExpress (MCE)

Cat. No.HY-12624

CAS：1357470-29-1

Synonyms：ON123300

Purity：99.12%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Narazaciclib (ON123300), a strong and brain-penetrant multi-kinase inhibitor, inhibits CDK4 (IC50=3.9 nM), Ark5 (IC50=5 nM), PDGFRβ (IC50=26 nM), FGFR1 (IC50=26 nM), RET (IC50=9.2 nM), and FYN (IC50=11 nM). Single agent Narazaciclib causes a dose-dependent suppression of phosphorylation of Akt as well as activation of Erk in brain tumors. Narazaciclib inhibits CDK6 with an IC50 of 9.82 nM.

In Vitro：Narazaciclib (ON123300) inhibits U87 glioma cell proliferation with an IC50 of 3.4±0.1 μM[2]. Narazaciclib (1 and 10 μM) inhibits cell proliferation in a panel of 11 glioma models including a patient-derived model (GBM10)[2]. 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[2]. ON123300 inhibits PI3Kδ with the IC50 of 144nM[3].

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 (T1/2) is 1.5 h for 5 mg/kg and 25 mg/kg in plasma[2].

IC50 & Target：Cdk4/cyclin D1 3.9 nM (IC50) ARK5 5 nM (IC50) CDK6/cyclinD1 9.82 nM (IC50) RET 9.2 nM (IC50) FYN 11 nM (IC50) FGFR1 26 nM (IC50) PDGFRβ 26 nM (IC50) PI3K-δ 144 nM (IC50)

References：

[1]. Hua Lv, et al. Integrated pharmacokinetic-driven approach to screen candidate anticancer drugs for brain tumor chemotherapy. AAPS J. 2013 Jan;15(1):250-7. [Content Brief]

[2]. Xiaoping Zhang, et al. Preclinical pharmacological evaluation of a novel multiple kinase inhibitor, ON123300, in brain tumor models. Mol Cancer Ther. 2014 May;13(5):1105-16. [Content Brief]

[3]. S K A Divakar, et al. Dual inhibition of CDK4/Rb and PI3K/AKT/mTOR pathways by ON123300 induces synthetic lethality in mantle cell lymphomas. Leukemia. 2016 Jan;30(1):86-93. [Content Brief]

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MedChemExpress - Model Narazaciclib -1357470-29-1

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Narazaciclib