Firategrast
Based on 6 publication(s) in Google Scholar
Firategrast (SB 683699) is an orally active and specific α4β1/α4β7 integrin antagonist. Firategrast reduces trafficking of lymphocytes into the central nervous system (CNS) and decreases multiple sclerosis (MS) activity.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.75%
- No. CAS: 402567-16-2
- Fòrmula: C27H27F2NO6
- Peso molecular:499.50
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Firategrast
More- Immunity. 2024 Feb 13;57(2):364-378.e9. [Abstract]
- Clin Cancer Res. 2015 Oct 15;21(20):4642-51. [Abstract]
- Oncogene. 2022 Apr;41(16):2303-2314. [Abstract]
- Br J Pharmacol. 2020 Jun;177(12):2696-2711. [Abstract]
- PLoS Pathog. 2023 Dec 8;19(12):e1011860. [Abstract]
- J Cell Physiol. 2021 Mar;236(3):2156-2168. [Abstract]
Customer Validation & Images
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PK/PD Analysis
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Histological Imaging/Staining
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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Cell Migration/Invasion Assay
Actividad biológica
Descripciòn
|
α4β1 |
α4β7 |
In Vitro
Firategrast (0.1-10 μM; 1 hour) significantly reduces chronic lymphocytic leukemia (CLL) cells adhesion[2].
Firategrast is a potent Integrin α4β1 (VLA-4) antagonist (IC50=198 nM) at inhibiting the binding of soluble VCAM/Fc chimeric protein (sVCAM-1) to G2 acute lymphoblastic leukemia (ALL) cells. VLA-4 is composed of CD49d (α4) and CD29 (β1)[1][4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Wild-type C57BL/6J mice (8-12 weeks) with primary TCL1-tg splenocytes[3]
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Dosage:30 mg/kg
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Administration:Drinking water; daily; starting 2 or 7 days post transplantation to 21 days
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Result:Showed an overall reduction of leukemic cells in the spleen, accompanied by significant spleen weight reduction.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 402567-16-2
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Appearance Solid
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Peso molecular 499.50
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Fòrmula C27H27F2NO6
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Color White to off-white
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SMILES
O=C(O)[C@@H](NC(C1=C(F)C=CC=C1F)=O)CC2=CC=C(C3=C(OC)C=C(COCC)C=C3OC)C=C2
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Synonyms
SB 683699
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (6)
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Journal Impact Factor
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Most Recent
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Immunity
Small-molecule CBP/p300 histone acetyltransferase inhibition mobilizes leukocytes from the bone marrow via the endocrine stress response. [Abstract]2024 Feb 13;57(2):364-378.e9. PMID: 38301651
Firategrast purchased from MedChemExpress. Usage Cited in: Immunity. 2024 Feb 13;57(2):364-378.e9. [Abstract]
Dynamic changes in blood leukocytes and neutrophils upon Firategrast (50 mg/kg) or vehicle treatment expressed as percentage of the mean cell count at baseline.
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Clin Cancer Res
Treatment with Ibrutinib Inhibits BTK- and VLA-4-Dependent Adhesion of Chronic Lymphocytic Leukemia Cells In Vivo. [Abstract]2015 Oct 15;21(20):4642-51. PMID: 26089373
Firategrast purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2015 Oct 15;21(20):4642-51. [Abstract]
Firategrast (FIR, 500 nM; 1 h) significantly reduced the adhesion of CLL cells to fibronectin in CLL peripheral blood mononuclear cells (PBMCs) (median change -32%, interquartile range: -13 to -44, n=15, P=0.001).
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Oncogene
Loss of IRF7 accelerates acute myeloid leukemia progression and induces VCAM1-VLA-4 mediated intracerebral invasion. [Abstract]2022 Apr;41(16):2303-2314. PMID: 35256780
Firategrast purchased from MedChemExpress. Usage Cited in: Oncogene. 2022 Apr;41(16):2303-2314. [Abstract]
The mice were intravenously injected with an equal number of AML-IRF7−/− cells followed by daily administration of Firategrast (20 mg/kg/day; oral gavage) or not. The mice were sacrificed when PB GFP+ cells reached 20%. Representative results of HE-stained brain sections are shown. Scale bars, 100 or 50 μm.
Firategrast purchased from MedChemExpress. Usage Cited in: Oncogene. 2022 Apr;41(16):2303-2314. [Abstract]
The mice were intravenously injected with an equal number of AML-IRF7−/− cells followed by daily administration with or without Firategrast (20 mg/kg/day; oral gavage). The percentage of peripheral blood AML cells was monitored every 5 days (n = 5). The results showed that, starting from day 10, the level of peripheral blood AML cells decreased in mice treated with Fragrastar.
Firategrast purchased from MedChemExpress. Usage Cited in: Oncogene. 2022 Apr;41(16):2303-2314. [Abstract]
The mice were intravenously injected with an equal number of AML-IRF7−/− cells followed by daily administration with or without Firategrast (20 mg/kg/day; oral gavage). The survival of mice is shown in Kaplan–Meier curves (n = 10). The results showed that Firastrast treatment prolonged the survival of AML-IRF7−/− mice.
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Br J Pharmacol
2020 Jun;177(12):2696-2711. PMID: 31985813 -
PLoS Pathog
2023 Dec 8;19(12):e1011860. PMID: 38064524 -
J Cell Physiol
Positive effect of Astragaloside IV on neurite outgrowth via talin-dependent integrin signaling and microfilament force. [Abstract]2021 Mar;236(3):2156-2168. PMID: 32853433
Solvente y solubilidad
In Vitro:
DMSO : ≥ 100 mg/mL (200.20 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Ethanol : ≥ 50 mg/mL (100.10 mM)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 1% SBE-β-CD in Saline
Solubility: 0.2 mg/mL (0.40 mM); Clear solution; Need ultrasonic and warming
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[2]. Sarah E M Herman, et al. Treatment with Ibrutinib Inhibits BTK- and VLA-4-Dependent Adhesion of Chronic Lymphocytic Leukemia Cells In Vivo. Clin Cancer Res. 2015 Oct 15;21(20):4642-51. [Content Brief]
[3]. Eva Szenes, et al. TCL1 transgenic mice as a model for CD49d-high chronic lymphocytic leukemia. Leukemia. 2020 Sep;34(9):2498-2502. [Content Brief]
[4]. H Rahimi, et al. Aberrant regulation of the integrin very late antigen-4 in systemic lupus erythematosus. Lupus. 2013 Mar;22(3):297-306. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| Ethanol / DMSO | 1 mM | 2.0020 mL | 10.0100 mL | 20.0200 mL | 50.0501 mL |
| 5 mM | 0.4004 mL | 2.0020 mL | 4.0040 mL | 10.0100 mL | |
| 10 mM | 0.2002 mL | 1.0010 mL | 2.0020 mL | 5.0050 mL | |
| 15 mM | 0.1335 mL | 0.6673 mL | 1.3347 mL | 3.3367 mL | |
| 20 mM | 0.1001 mL | 0.5005 mL | 1.0010 mL | 2.5025 mL | |
| 25 mM | 0.0801 mL | 0.4004 mL | 0.8008 mL | 2.0020 mL | |
| 30 mM | 0.0667 mL | 0.3337 mL | 0.6673 mL | 1.6683 mL | |
| 40 mM | 0.0501 mL | 0.2503 mL | 0.5005 mL | 1.2513 mL | |
| 50 mM | 0.0400 mL | 0.2002 mL | 0.4004 mL | 1.0010 mL | |
| 60 mM | 0.0334 mL | 0.1668 mL | 0.3337 mL | 0.8342 mL | |
| 80 mM | 0.0250 mL | 0.1251 mL | 0.2503 mL | 0.6256 mL | |
| 100 mM | 0.0200 mL | 0.1001 mL | 0.2002 mL | 0.5005 mL |
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