ON123300

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ON123300

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1357470-29-1

包装与价格：

包装	价格(元)
5mg	电议
25mg	电议

产品介绍

ON123300，一种强效的脑渗透性多激酶抑制剂，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)。单剂 ON123300 导致脑肿瘤中 Akt 磷酸化和 Erk 激活的剂量依赖性抑制。 ON123300 抑制 CDK6，IC50 为 9.82 nM。

Cas No.	1357470-29-1
别名	8-环戊基-7,8-二氢-2-[[4-(4-甲基-1-哌嗪基)苯基]氨基]-7-氧代-吡啶并[2,3-D]嘧啶-6-甲腈,ON123300
化学名	8-cyclopentyl-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carbonitrile
Canonical SMILES	N#CC1=CC2=CN=C(NC3=CC=C(N4CCN(C)CC4)C=C3)N=C2N(C5CCCC5)C1=O
分子式	C₂₄H₂₇N₇O
分子量	429.52
溶解度	≥ 21.5mg/mL in DMSO with gentle warming
储存条件	Store at -20℃
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	IC50: 3.9, 5, 26, 26, 9.2 and 11 nM for CDK4, Ark5, PDGFRβ, FGFR1, RET, and Fyn, respectively. ON123300 is a multi-targeted kinase inhibitor. The signaling hyperactivation of RTK is most commonly caused by EGFR mutation/amplification or PDGFR amplification/overexpression. FGFR1signaling also occurs in GBM exhibiting FGFR1 kinase domain gain-of-function mutations. In vitro: In previous study, when Z138C and Granta 519 cells were treated with ON123300, it was found that ON123300 was efficient to inhibit the phosphorylation of Rb family proteins. Moreover, ON123300 was able to inhibit the phosphorylation of proteins that were involved in the PI3K/AKT pathway. In addition, ON123300-treated cells similarly arrested at lower concentrations, however, higher concentrations could lead to the apoptosis induction [1]. In vivo: Previous animal in vivo study showed that mouse xenograft had a strong inhibition of MCL tumor growth in ON123300-treated animals. Moreover, the treatment with ON123300 to ibrutinib-sensitive and -resistant patient-derived MCLs was able to trigger apoptosis and inhibition of both Rb and PI3K/AKT pathways, indicating that ON123300 could be an effective drug in the treatment of MCL, such as ibrutinib-resistant forms of the disease [1]. Clinical trial: Up to now, ON12300 is still in the preclinical development stage. Reference: [1] Divakar SK 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.