| Size | Price | Stock | Qty |
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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 |
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Purity: ≥98%
Tanzisertib HCl (also known as CC-930) is a potent, specific and and orally bioavailable JNK1/JNK2/JNK3 inhibitor that has the potential to be used for the treatment of fibrotic and infammatory indications. CC-930 is potent against all isoforms of JNK [Ki(JNK1) = 44 ± 3 nM, IC50(JNK1) = 61 nM, Ki(JNK2) = 6.2 ± 0.6 nM, IC50(JNK2) = 5 nM, IC50(JNK3) = 5 nM] and selective against MAP kinases ERK1 and p38a with IC50 values of 3.4 μM For the prevention and treatment of dermal fibrosis, tanzisertib is currently undergoing a Phase 1 clinical trial.
| ln Vitro |
Tanzisertib (CC-930) inhibits the synthesis of phospho-cJun in human PBMC stimulated by phorbol-12-myristate-13-acetate and phytohemeagglutinin (IC50=1 μM)[1]. In FC-loaded WT hepatocytes, tanzisertib (CC-930) (1-2 μM) completely abolishes apoptosis and necrosis[2]. In systemic sclerosis, tanzisertib (CC-930) inhibits the JNK pathway that is triggered by pro-fibrotic cytokines[3].
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| ln Vivo |
Tanzisertib (CC-930) (10 and 30 mg/kg, p.o.) inhibits the production of TNFa by 23% and 77% in the acute rat LPS-induced TNFa production PK-PD model[1]. Tanzisertib (CC-930) (150 mg/kg) can cause the regression of pre-existing fibrosis while also preventing the development of fibrosis in various models[3].
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| Enzyme Assay |
CC-930 is kinetically competitive with ATP in the JNK-dependent phosphorylation of the protein substrate c-Jun and potent against all isoforms of JNK [Ki(JNK1) = 44 ± 3 nM, IC50(JNK1) = 61 nM, Ki(JNK2) = 6.2 ± 0.6 nM, IC50(JNK2) = 5 nM, IC50(JNK3) = 5 nM] and selective against MAP kinases ERK1 and p38a with IC50 of 0.48 and 3.4 μM respectively.
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| Cell Assay |
In 96-well plates with 1 µM Tanzisertib (CC-930), fibroblasts from patients with systemic sclerosis (SSc) are incubated for 20 hours. The cells are then given an additional 4 hours of incubation at 37°C before receiving MTT at a final concentration of 1 mg/mL. All other results are normalized to untreated cells while mock-treated fibroblasts serve as the standard.
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| Animal Protocol |
A modified version of the bleomycin-induced dermal fibrosis model is used to assess the regression of fibrosis on inhibition of JNK. In this model, significant dermal fibrosis is already present three weeks after the start of the challenge and is treated with bleomycin. The results of six different groups, comprising a total of 40 mice, are analyzed. NaCl is subcutaneously injected into the first group of mice for a total of six weeks. In order to assess the level of fibrosis prior to treatment and to prevent spontaneous fibrosis regression, the second group receives injections of bleomycin for 3 weeks, followed by injections of NaCl for an additional 3 weeks. After six weeks of bleomycin injections, the third group of mice is euthanized. The final three weeks of a continuous six-week challenge with bleomycin are spent administering Tanzisertib (CC-930) to the fourth and fifth groups at doses of 50 mg/kg and 150 mg/kg, respectively. The sixth group is a positive control group made up of mice that were given bleomycin for six weeks before being given imatinib at a dose of 50 mg/kg for the final three weeks.
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| References |
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| Molecular Formula |
C21H23F3N6O2
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| Molecular Weight |
448.441534280777
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| CAS # |
899805-25-5
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| Related CAS # |
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| SMILES |
N(C1C(F)=CC(F)=CC=1F)C1=NC2C=NC(=NC=2N1[C@@H]1COCC1)N[C@@H]1CC[C@@H](O)CC1
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2300 mL | 11.1498 mL | 22.2995 mL | |
| 5 mM | 0.4460 mL | 2.2300 mL | 4.4599 mL | |
| 10 mM | 0.2230 mL | 1.1150 mL | 2.2300 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.
Bioorg Med Chem Lett.2012 Feb 1;22(3):1433-8. |
Bioorg Med Chem Lett.2012 Feb 1;22(3):1433-8. |
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