DB07268 |
Catalog No.GC14114
One-Click Copy Product Info
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A potent inhibitor of JNK1
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 929007-72-7
Sample solution is provided at 25 µL, 10mM.
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IC50: 9 nM for JNK1
DB07268 is a JNK1 inhibitor. The c-Jun N-terminal kinases (JNKs) are members of the mitogen-activated protein kinase family. Three JNK isoforms (JNK1, 2 and 3) have been identified. There is growing evidences indicating that activation of the JNK activity is involved in a number of human disease settings. Therefore, considerable efforts have been directed toward the identification of JNK inhibitors suitable for clinical development.
In vitro: The selectivity data of DB07268 against a panel of kinases has been tested. Results showed that DB07268 had some degree of selectivity over quite a few kinases with the exceptions of PLK, CHK1, and CK2. Although d DB07268 showed submicromolar potency against these three kinases, it still appeared to exhibit at least 70- to 90-fold greater potency against JNK1 than PLK, CHK1, and CK2 [1].
In vivo: Several analogs of DB07268 were profiled in vivo. These compounds had a range of exposure in rats and mice. Some had excellent brain penetration despite having poor rat pharmacokinetics, while others had a more balanced profile. Unfortunately, the most potent analog exhibited poor rat pk demonstrated by a short half-life, low oral absorption and poor brain penetration. One DB07268 analog likely exhibited modest rat pk with low clearance and decent oral absorption. This analog also showed modest brain penetration [1].
Clinical trial: So far, no clinical study has been reported.
References:
[1] Liu M,Wang S,Clampit JE,Gum RJ,Haasch DL,Rondinone CM,Trevillyan JM,Abad-Zapatero C,Fry EH,Sham HL,Liu G. Discovery of a new class of 4-anilinopyrimidines as potent c-Jun N-terminal kinase inhibitors: Synthesis and SAR studies. Bioorg Med Chem Lett.2007 Feb 1;17(3):668-72. Epub 2006 Nov 2.
[2] Romain Nol, Youseung Shin, Xinyi Song, Yuanjun He, Marcel Koenig, Weimin Chen, Yuan Yuan Ling, Li Lin, Claudia H. Ruiz, Phil LoGrasso, Michael D. Cameron, Derek R. Duckett, Theodore M. Kamenecka. Synthesis and SAR of 4-(pyrazol-3-yl)-pyridines as novel c-Jun N-terminal kinase inhibitors.Bioorg Med Chem Lett. 2011 May 1; 21(9): 2732–2735.
| Cas No. | 929007-72-7 | SDF | |
| Chemical Name | 2-[[2-(3-hydroxyanilino)pyrimidin-4-yl]amino]benzamide | ||
| Canonical SMILES | C1=CC=C(C(=C1)C(=O)N)NC2=NC(=NC=C2)NC3=CC(=CC=C3)O | ||
| Formula | C17H15N5O2 | M.Wt | 321.33 |
| Solubility | ≥ 15.2 mg/mL in DMSO | 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 | 3.1121 mL | 15.5603 mL | 31.1207 mL |
| 5 mM | 622.4 μL | 3.1121 mL | 6.2241 mL |
| 10 mM | 311.2 μL | 1.556 mL | 3.1121 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: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)