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Purity: ≥98%
SB-265610 is a novel, potent, selective, nonpeptide, competitive, and allosteric CXCR2 antagonist that inhibits CINC-1-mediated but not C5a-mediated Ca2+ mobilization (IC50 are 3.4 and 6800 nM respectively). It inhibits CINC-induced chemotaxis and attenuates neutrophil accumulation in inflammatory lung injury in vivo. SB-265610 blocks rat cytokine-induced neutrophil chemoattractant-1 (CINC-1)-induced calcium mobilization and neutrophil chemotaxis with IC50s of 3.7 nM and 70 nM, respectively.
| ln Vitro |
SB-265610 has an IC50 of 3.7 nM for cytokine-induced neutrophil chemoattractant-1 (CINC-1) activation, and an IC50 of 70 nM for concentration-dependent neutrophil chemotaxis. When CINC-1 is administered at levels not previously attained, SB-265610 diminishes the anti-cellular effects of CINC-1 [1].
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| ln Vivo |
SB-265610 therapy (2 mg/kg/day; i.p.; daily; continued in the afternoon) significantly reduced Gr-1+CD11b+ cell recruitment to Tgfbr2 breast cancer, but did not affect blank tumors [3].
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| Animal Protocol |
Animal/Disease Models: MMTV-PyVmT/Tgfbr2MGKO and MMTV-PyVmT/Tgfbr2flox/flox tumors from donor mice [3]
Doses: 2 mg/kg/day Doses: Intraperitoneal; Daily; Two-week Experimental Results: Significant Inhibits the recruitment of Gr-1+CD11b+ cells to breast cancer. |
| References |
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| Molecular Formula |
C14H9BRN6O
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|---|---|
| Molecular Weight |
357.164860486984
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| Exact Mass |
356.002
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| Elemental Analysis |
C, 47.08; H, 2.54; Br, 22.37; N, 23.53; O, 4.48
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| CAS # |
211096-49-0
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| PubChem CID |
9841667
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.779 g/cm3
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| Boiling Point |
527ºC at 760 mmHg
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| Flash Point |
272.5ºC
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| LogP |
3.382
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
22
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| Complexity |
466
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
SEDUMQWZEOMXSO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H9BrN6O/c15-9-3-1-2-4-10(9)17-14(22)18-11-6-5-8(7-16)12-13(11)20-21-19-12/h1-6H,(H2,17,18,22)(H,19,20,21)
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| Chemical Name |
N-(2-Bromophenyl)-N'-(7-cyano-1H-benzotriazol-4-yl)urea
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| Synonyms |
SB-265610 SB 265610 SB265610.
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| HS Tariff Code |
2934.99.03.00
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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 : ~50 mg/mL (~139.99 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.00 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 (7.00 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7999 mL | 13.9993 mL | 27.9987 mL | |
| 5 mM | 0.5600 mL | 2.7999 mL | 5.5997 mL | |
| 10 mM | 0.2800 mL | 1.3999 mL | 2.7999 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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