| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| 500mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
JNK1 (IC50 = 9 nM); CHK1 (IC50 = 0.82 nM); PAK4 (IC50 = 5.5 μM); AKT1 (IC50 = 15 μM); ERK2 (IC50 = 25 μM)
JNK1 (c-Jun N-terminal kinase 1). IC50 = 9 nM. |
|---|---|
| ln Vitro |
DB07268 (Compound 2b) also inhibits CHK1, PAK4, AKT1, and ERK2 with respective IC50 values of 0.82 μM, 5.5 μM, 15 μM, and 25 μM, respectively[1].
DB07268 is a potent and selective ATP-competitive JNK1 inhibitor. With an IC50 of 9 nM, it inhibits JNK1 activity. It exhibits at least 70- to 90-fold selectivity over CHK1, CK2, and PLK. By inhibiting JNK1, it modulates JNK1-driven profibrotic pathways. |
| ln Vivo |
In vivo, DB07268 has been validated in colorectal cancer organoid models, showing selective activity in APC-mutated contexts. It has also been studied in autophagy studies via the JNK1/TSC2 axis. It is used to study JNK1-specific signaling pathways in disease models.
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| Enzyme Assay |
DB07268 is evaluated in cell-free kinase assays using purified JNK1 enzyme. The compound is incubated with JNK1, ATP, and a substrate, and the inhibition of kinase activity is measured. IC50 values are determined to quantify the potency of JNK1 inhibition. Selectivity is assessed by screening against a panel of kinases.
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| Cell Assay |
DB07268 is assessed in cell-based assays using fibroblast, myofibroblast, or cancer cell lines. Cells are treated with DB07268, and JNK1 activity is measured by assessing phosphorylation of downstream substrates. Functional readouts, such as cell proliferation, migration, or apoptosis, may also be assessed.
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| Animal Protocol |
DB07268 is administered in animal models, including colorectal cancer organoid models and xenografts. Efficacy is assessed by measuring tumor growth inhibition or modulation of JNK1 signaling pathways. Pharmacokinetic studies are conducted to assess bioavailability and tissue distribution.
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| ADME/Pharmacokinetics |
No detailed PK data available. DB07268 has a molecular weight of 321.33. Soluble in DMSO (≥32 mg/mL). Purity ≥98%. Storage at -20°C.
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| Toxicity/Toxicokinetics |
No detailed toxicity data available. For research use only.
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| References | |
| Additional Infomation |
2-({2-[(3-hydroxyphenyl)amino]pyrimidin-4-yl}amino)benzamide is an aminopyrimidine compound belonging to the benzamide class. It acts as a protein kinase inhibitor.
DB07268 is a potent and selective JNK1 inhibitor. Molecular formula: C17H15N5O2; MW: 321.33. IC50 = 9 nM. For research use only. |
| Molecular Formula |
C17H15N5O2
|
|---|---|
| Molecular Weight |
321.333302736282
|
| Exact Mass |
321.122
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| Elemental Analysis |
C, 63.54; H, 4.71; N, 21.79; O, 9.96
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| CAS # |
929007-72-7
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| Related CAS # |
929007-72-7
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| PubChem CID |
16058637
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| Appearance |
White to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
641.6±65.0 °C at 760 mmHg
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| Flash Point |
341.8±34.3 °C
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| Vapour Pressure |
0.0±2.0 mmHg at 25°C
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| Index of Refraction |
1.753
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| LogP |
1.96
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
24
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| Complexity |
422
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(C1C(NC2C=CN=C(NC3C=C(O)C=CC=3)N=2)=CC=CC=1)N
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| InChi Key |
QHPKKGUGRGRSGA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H15N5O2/c18-16(24)13-6-1-2-7-14(13)21-15-8-9-19-17(22-15)20-11-4-3-5-12(23)10-11/h1-10,23H,(H2,18,24)(H2,19,20,21,22)
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| Chemical Name |
2-[[2-(3-hydroxyanilino)pyrimidin-4-yl]amino]benzamide
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| Synonyms |
DB 07268; DB07268; DB-07268
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ≥ 32 mg/mL (~99.6 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.47 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.47 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1121 mL | 15.5603 mL | 31.1207 mL | |
| 5 mM | 0.6224 mL | 3.1121 mL | 6.2241 mL | |
| 10 mM | 0.3112 mL | 1.5560 mL | 3.1121 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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