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| 25mg |
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Purity: ≥98%
CEP33779 is a novel, potent, orally bioactive, highly selective inhibitor of JAK2 (Janus kinase) with potential antitumor and anti-inflammatory activity. It inhibits JAK2 with an IC50 of 1.8 nM, and exhibits >40- and >800-fold selectivity for JAK2 over JAK1 and TYK2. CEP33779 showed high activity in mice with collagen-induced arthritis (CIA) and collagen-antibody induced arthritis (CAIA). It induced regression of established colorectal tumors, reduced angiogenesis, and reduced proliferation of tumor cells. The ability of CEP-33779 to suppress growth of colorectal tumors by inhibiting the IL-6/JAK2/STAT3 signaling suggests a potential therapeutic utility of JAK2 inhibitors in multiple tumors types, particularly those with a strong inflammatory component.
| ln Vitro |
At non-toxic concentrations, P-glycoprotein-overexpressing multidrug-resistant cells' overexpression sensitivity to CEP-33779's anti-cancer substrates is markedly increased. Through inhibition of P-glycoprotein transport function overexpression, CEP-33779 drastically lowers doxorubicin efflux and increases intracellular accumulation [3].
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| ln Vivo |
In nude mice, CEP-33779 showed a good PK profile with an intravenous half-life of one hour, a moderate distribution (Vd=2.6 L/kg), and a detectable oral exposure with an estimated 33% bioavailability. In the CWR22 xenograft model, it demonstrated antitumor efficacy; oral administration at 30 mg/kg bid for 14 days led to tumor stasis and partial regression in 5/10 animals [1]. Most animals that received CEP-33779 had almost total tumor shrinkage; the few tumor nodules that remained were tiny, poorly vascularized, and appeared necrotic. Tumor-associated NF-κB activation is inhibited by CEP-33779 [2].
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| References |
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| Molecular Formula |
C24H26N6O2S
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| Molecular Weight |
462.57
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| Exact Mass |
462.183
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| CAS # |
1257704-57-6
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| Related CAS # |
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| PubChem CID |
57336812
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.693
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| LogP |
2.02
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
33
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| Complexity |
745
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
RFZKSQIFOZZIAQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H26N6O2S/c1-28-13-15-29(16-14-28)20-6-3-5-19(17-20)25-24-26-23-22(7-4-12-30(23)27-24)18-8-10-21(11-9-18)33(2,31)32/h3-12,17H,13-16H2,1-2H3,(H,25,27)
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| Chemical Name |
N-(3-(4-methylpiperazin-1-yl)phenyl)-8-(4-(methylsulfonyl)phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-amine
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| Synonyms |
CEP-33779; CEP 33779; CEP33779
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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 Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.40 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 25.0 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: ≥ 2.5 mg/mL (5.40 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 25.0 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.40 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 1% DMSO+30% polyethylene glycol+1% Tween 80:30 mg/mL Solubility in Formulation 5: 10 mg/mL (21.62 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1618 mL | 10.8092 mL | 21.6183 mL | |
| 5 mM | 0.4324 mL | 2.1618 mL | 4.3237 mL | |
| 10 mM | 0.2162 mL | 1.0809 mL | 2.1618 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.
JAK2 blockade ameliorates collagen antibody-induced arthritis (CAIA) paw inflammation.Arthritis Res Ther.2011 Apr 21;13(2):R68. |
JAK2 blockade reduces several disease correlates in a model of chronic degenerative arthritis.Arthritis Res Ther.2011 Apr 21;13(2):R68. |
Suppression of carrageenan-induced inflammation by CEP-33779. Arthritis Res Ther. 2011; 13(2): R68.Arthritis Res Ther.2011 Apr 21;13(2):R68. |
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