PLX647 is a dual inhibitor of the receptor tyrosine kinases FMS and KIT, selectively targeting these proteins with high specificity and potency. It demonstrates inhibitory effects on the proliferation of cells expressing constitutively active FMS or KIT, as well as ligand-dependent growth of cells with endogenous FMS and KIT. Additionally, PLX647 has been shown to inhibit differentiation of human osteoclast precursor cells and reduce inflammation and bone destruction in various animal models.
873786-09-5
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Basic information
- Product Name: PLX647
- Synonyms: PLX647;PLC647;5-(1H-Pyrrolo[2,3-b]pyridin-3-ylmethyl)-N-[[4-(trifluoromethyl)phenyl]methyl]-2-pyridinamine;[5-[(1H-Pyrrolo[2,3-b]pyridin-3-yl)methyl]pyridin-2-yl](4-trifluoromethylbenzyl)amine
- CAS NO:873786-09-5
- Molecular Formula: C21H17F3N4
- Molecular Weight: 382.3816896
- EINECS: N/A
- Product Categories: Inhibitors
- Mol File: 873786-09-5.mol
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Chemical Properties
- Melting Point: N/A
- Boiling Point: N/A
- Flash Point: N/A
- Appearance: white to beige/
- Density: N/A
- Refractive Index: N/A
- Storage Temp.: 2-8°C
- Solubility: DMSO: soluble20mg/mL, clear
- CAS DataBase Reference: PLX647(CAS DataBase Reference)
- NIST Chemistry Reference: PLX647(873786-09-5)
- EPA Substance Registry System: PLX647(873786-09-5)
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Safety Data
- Hazard Codes: Xi
- Statements: 36/37/38
- Safety Statements: 36/37/39
- WGK Germany: 3
- RTECS:
- HazardClass: N/A
- PackingGroup: N/A
- Hazardous Substances Data: 873786-09-5(Hazardous Substances Data)
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873786-09-5 Usage
Uses
Used in Oncology:PLX647 is used as a tyrosine kinase inhibitor for targeting c-Kit and c-Fms in cancer treatment. Its selectivity for these kinases makes it a promising candidate for the treatment of malignancies driven by the dysregulation of FMS and KIT, potentially leading to the inhibition of tumor growth and progression.
Used in Inflammatory Conditions:
PLX647 is used as an anti-inflammatory agent for reducing the release of pro-inflammatory cytokines such as TNF-α and IL-6 in animal models of inflammation. This application may be beneficial in treating conditions characterized by excessive inflammation, such as autoimmune diseases.
Used in Allergy and Immune Responses:
PLX647 is used as a therapeutic agent for inhibiting mast cell degranulation in mouse models of passive cutaneous anaphylaxis (PCA). This suggests its potential use in treating allergic reactions and modulating immune responses.
Used in Bone Diseases:
PLX647 is used as a bone protective agent for inhibiting bone destruction and delaying disease progression in mouse models of collagen-induced arthritis (CIA). It also reverses bone osteolysis and allodynia in a syngeneic rat model of cancer-induced bone pain, indicating its potential use in treating bone-related diseases and conditions associated with pain and bone loss.
references
[1]. zhang c, ibrahim pn, zhang j, et al. design and pharmacology of a highly specific dual fms and kit kinase inhibitor. proc natl acad sci u s a, 2013, 110(14): 5689-5694.Check Digit Verification of cas no
The CAS Registry Mumber 873786-09-5 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,7,3,7,8 and 6 respectively; the second part has 2 digits, 0 and 9 respectively.Calculate Digit Verification of CAS Registry Number 873786-09:
(8*8)+(7*7)+(6*3)+(5*7)+(4*8)+(3*6)+(2*0)+(1*9)=225
225 % 10 = 5
So 873786-09-5 is a valid CAS Registry Number.
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