MLN3897
MLN3897 is an orally active CCR1 antagonist. MLN3897 inhibits the c-fos and Akt pathways by blocking the binding of CCL3 to CCR1, thereby reducing immune cell infiltration, attenuating osteoclasts, and interfering with tumor-microenvironment interactions. MLN3897 can be used in research on multiple myeloma, multiple myeloma bone disease, and rheumatoid arthritis.
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- CAS. Nr.: 690660-17-4
- Formel: C30H31ClN2O4
- Molecular Weight:519.03
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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- Reinheit & Dokumentation
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Biologische Aktivität
Beschreibung
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CCR1 |
c-Fos |
Akt |
In Vitro
MLN3897 (10 nM) impairs osteoclast formation and function in myeloma cell models and inhibits the survival and proliferation of multiple myeloma cells[4].
MLN3897 impairs osteoclast formation and function in multiple myeloma by reducing precursor cell multinucleation and downregulating c-fos signaling; by inhibiting the Akt signaling pathway, it blocks CCL-3 (HY-P7256)-induced multiple myeloma cell migration and can inhibit the adhesion of multiple myeloma cells to osteoclasts[3].
MLN3897 inhibits CCL3-induced CD11b upregulation in human whole blood monocytes with an IC50 of 210 nM[2].
MLN3897 inhibits CCR1-mediated internalization of Alexa647-CCL3 in human whole blood with an IC50 of 45 nM[2].
MLN3897 potently inhibits CCL15 (HY-P7266)-induced chemotaxis of freshly isolated human monocytes in 100% human serum, with an IC50 of 2 nM[2].
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:SCID (humanized model, SCID-hu)[1]
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Dosage:2 mg/kg
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Administration:p.o.; once daily; 4 weeks
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Result:Decreased shIL6R levels in treated mice.
Reduced tumor infiltration to 26% versus 40% in vehicle controls.
Decreased osteoclast number per bone area to 29 versus 46.2 in controls.
Increased trabecular area/bone area (TA/BA) to 27 versus 15.9 in controls.
Observed osteoblast number per mm2 bone of 506 versus 575 in controls.
Increased osteocalcin-positive area/trabecular area (OCN+/TA) to 0.53 versus 0.26 in controls.
Chemical Information
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CAS. Nr. 690660-17-4
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Molecular Weight 519.03
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Formel C30H31ClN2O4
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SMILES
CC(C)([C@](CC1)(C2=CC=C(C=C2)Cl)O)CN1CC/C=C3C4=CC(C(O)=O)=CC=C4OCC5=NC=CC=C5/3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Vallet S, et al. CCR1 as a target for multiple myeloma. Expert opinion on therapeutic targets. 2011 Sep;15(9):1037-47. [Content Brief]
[2]. Dairaghi DJ, et al. Pharmacokinetic and pharmacodynamic evaluation of the novel CCR1 antagonist CCX354 in healthy human subjects: implications for selection of clinical dose. Clinical pharmacology and therapeutics. 2011 May;89(5):726-34. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
MLN3897 Related Classifications
HY-15544A Related Classifications
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