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Purity: ≥98%
NBI-74330 (NBI74330) is a novel, potent and selective antagonist for CXCR3 (CXC chemokine receptor 3) with potential anticancer, immunomodulatory and antiinflammatory activities. It shows strong inhibition of (125I)CXCL10 and (125I)CXCL11 specific binding with Ki of 1.5 and 3.2 nM, respectively, and inhibits CXCR3 with IC50 values ranging from 7 to 18 nM. In mice lacking the LDL receptor, NBI-74330 reduces the development of atherosclerotic plaque. Glioma growth is stimulated by the chemokine receptor CXCR3. Since CXCR3 antagonism directly inhibits gliomas, treating human GBM may benefit from targeting this receptor as a therapeutic target.
Targets |
[125I]CXCL10-CXCR3 ( Ki = 1.5 nM ); [125I]CXCL11-CXCR3 ( Ki = 3.2 nM )
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ln Vitro |
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ln Vivo |
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Enzyme Assay |
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Animal Protocol |
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References |
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Molecular Formula |
C32H27F4N5O3
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Molecular Weight |
605.5821
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Exact Mass |
605.21
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Elemental Analysis |
C, 63.47; H, 4.49; F, 12.55; N, 11.56; O, 7.93
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CAS # |
855527-92-3
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Related CAS # |
473722-68-8 (racemate);855527-92-3 (R-isomer)
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Appearance |
Solid powder
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SMILES |
CCOC1=CC=C(C=C1)N2C(=O)C3=C(N=CC=C3)N=C2C(C)N(CC4=CN=CC=C4)C(=O)CC5=CC(=C(C=C5)F)C(F)(F)F
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InChi Key |
XMRGQUDUVGRCBS-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C32H27F4N5O3/c1-3-44-24-11-9-23(10-12-24)41-30(39-29-25(31(41)43)7-5-15-38-29)20(2)40(19-22-6-4-14-37-18-22)28(42)17-21-8-13-27(33)26(16-21)32(34,35)36/h4-16,18,20H,3,17,19H2,1-2H3
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Chemical Name |
N-[1-[3-(4-ethoxyphenyl)-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-2-[4-fluoro-3-(trifluoromethyl)phenyl]-N-(pyridin-3-ylmethyl)acetamide
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Synonyms |
NBI74330; NBI 74330; NBI-74330.
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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: ~100 mg/mL (~165.1 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (4.13 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 (4.13 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 (4.13 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.6513 mL | 8.2565 mL | 16.5131 mL | |
5 mM | 0.3303 mL | 1.6513 mL | 3.3026 mL | |
10 mM | 0.1651 mL | 0.8257 mL | 1.6513 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.
The selectivity and specificity of a murine CXCR3 internalization assay.Br J Pharmacol. 2007 Dec; 152(8): 1260–1271. th> |
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PK/PD parameters of NBI-74330 (100 mg kg−1) following oral administration to mice. PK/PD parameters of NBI-74330 (100 mg kg−1) following subcutaneous administration to mice.Br J Pharmacol. 2007 Dec; 152(8): 1260–1271. td> |
Murine CXCR3 receptor classification using receptor internalization and GTPγS assays. Tolerance of the murine CXCR3 internalization assay to plasma.Br J Pharmacol. 2007 Dec; 152(8): 1260–1271. td> |