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Purity: ≥98%
CEP-1347 (also known as KT7515), a derivative of the natural product K-252a found in broths of Narcodiopsis bacterium, is a novel, potent and mixed lineage kinase inhibitor (mainly JNK) with IC50 of 30 nM on JNK1. It demonstrates neuroprotective properties and has the potential for the treatment of neurodegenerative diseases such as PD. CEP-1347 promotes neuronal survival at dosages that inhibit activation of JNKs in primary embryonic cultures. CEP-1347 is tested in a large-scale phase 2/3 clinical trial in early Parkinson's disease, in which its safety and tolerability, but nevertheless not efficacy, was demonstrated. . In addition, CEP-1347 has been reported as a promising candidate for cancer stem cell-targeting therapy and that further clinical and preclinical studies are warranted to evaluate its efficacy in cancer treatment.
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| References |
:Anticancer Res.2018 Aug;38(8):4535-4542;Oncotarget.2017 Oct 24;8(55):94872-94882.
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| Additional Infomation |
CEP-1347 is a semi-synthetic compound shown to protect multiple nerve cell types from a variety of insults leading to programmed cell death (apoptosis) which could improve the survival of dopamine neurons prior to and after transplantation.
Drug Indication Investigated for use/treatment in asthma and parkinson's disease. Mechanism of Action CEP-1347, an orally active molecule, is a selective and potent inhibitor of the stress-activated protein kinase pathway, an intracellular signaling pathway that is an essential component of the stress response leading to neuronal death. In-vitro cell culture systems and in-vivo mouse and non-human primate models of Parkinson's disease have shown that CEP-1347 protects dopamine neurons in the substantia nigra, the area of the brain affected by Parkinson's disease. |
| Molecular Formula |
615.76
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| Molecular Weight |
C33H33N3O5S2
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| Exact Mass |
615.186
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| CAS # |
156177-65-0
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| Related CAS # |
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| PubChem CID |
9917013
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| Appearance |
White to off-white solid powder
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| LogP |
6.49
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
43
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| Complexity |
1150
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| Defined Atom Stereocenter Count |
3
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| SMILES |
CCSCC1=CC2=C(C=C1)N3[C@H]4C[C@@]([C@](O4)(N5C6=C(C=C(C=C6)CSCC)C7=C8CNC(=O)C8=C2C3=C75)C)(C(=O)OC)O
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| InChi Key |
SCMLRESZJCKCTC-KMYQRJGFSA-N
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| InChi Code |
InChI=1S/C33H33N3O5S2/c1-5-42-15-17-7-9-22-19(11-17)26-27-21(14-34-30(27)37)25-20-12-18(16-43-6-2)8-10-23(20)36-29(25)28(26)35(22)24-13-33(39,31(38)40-4)32(36,3)41-24/h7-12,24,39H,5-6,13-16H2,1-4H3,(H,34,37)/t24-,32+,33+/m1/s1
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| Chemical Name |
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| Synonyms |
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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 |
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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 Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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.
CEP-1347induces the differentiation of cancer stem cells into non-cancer stem cells.Oncotarget.2017 Oct 24;8(55):94872-94882. |
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CEP-1347treatment deprives cancer stem cells of their sphere forming ability.Cells treated without (Control) or withCEP-1347(300 nM for PANC-1 CSLC, 200 nM for the others) for 6 days were subjected to a sphere formation assay in the absence ofCEP-1347.Oncotarget.2017 Oct 24;8(55):94872-94882. |
Systemically administeredCEP-1347selectively targets and inhibits tumor-initiating cancer stem cells within tumors in tumor-bearing mice.Oncotarget.2017 Oct 24;8(55):94872-94882. |
CEP-1347inhibits the tumor-initiating capacity of cancer stem cells.Oncotarget.2017 Oct 24;8(55):94872-94882. |
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Short-term systemicCEP-1347treatment inhibits tumor formation by glioma stem cells in an orthotopic brain tumor model.Mice implanted intracranially with GS-Y03 cells underwent a daily i.p. injection ofCEP-1347(1.5 mg/kg/day) for 10 days.Oncotarget.2017 Oct 24;8(55):94872-94882. |
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