ON123300 |
Catalog No.GC15607
One-Click Copy Product Info
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multi-targeted kinase inhibitor,inhibits CDK4, Ark5, PDGFRβ, FGFR1, RET, and Fyn
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1357470-29-1
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 1357470-29-1 | SDF | |
| Chemical Name | 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 | ||
| Formula | C24H27N7O | M.Wt | 429.52 |
| Solubility | ≥ 21.5mg/mL in DMSO with gentle warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3282 mL | 11.6409 mL | 23.2818 mL |
| 5 mM | 465.6 μL | 2.3282 mL | 4.6564 mL |
| 10 mM | 232.8 μL | 1.1641 mL | 2.3282 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 20 reference(s) in Google Scholar.)