KBP-7018 hydrochloride
KBP-7018 hydrochloride is an orally active, tyrosine kinase-selective multi-kinase inhibitor with an IC50 value of 10 nM against c-KIT, 7.6 nM against RET, and 25 nM against human PDGFR. KBP-7018 hydrochloride improves survival rates in a mouse model of pulmonary fibrosis. KBP-7018 hydrochloride can be used in research related to idiopathic pulmonary fibrosis.
For research use only. We do not sell to patients.
- CAS No.: 1613437-67-4
- Formula: C31H31ClN4O5
- Molecular Weight:575.05
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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PDGFRβ 34 nM (IC50) |
PDGFRα 26 nM (IC50) |
CYP3A4 0.087 μM (IC50) |
KBP-7018 hydrochloride potently and selectively inhibits c-KIT (IC50 = 10 nM), RET (IC50 = 7.6 nM) and PDGFR (IC50 = 25 nM) in cell-free kinase assays. Meanwhile, it shows extremely weak inhibitory activity against hERG K+ and exhibits high kinome selectivity[1].
KBP-7018 hydrochloride inhibits h-PDGF-bb-stimulated proliferation of 3T3 fibroblasts in cell-based assays, with an IC50 of 100 nM[1].
KBP-7018 hydrochloride potently inhibits purified PDGFRα (IC50 = 26 nM) and PDGFRβ (IC50 = 34 nM)[2].
KBP-7018 (0.05-80 μM; 10 min) hydrochloride potently inhibits human CYP3A4 (testosterone probe, IC50 = 0.087 μM), weakly inhibits human CYP2C9 (IC50 = 35.2 μM), and shows no inhibitory effect on human CYP1A2, CYP2C19 or CYP2D6 at concentrations up to 80 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57 mice[1]
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Dosage:10 mg/kg; 30 mg/kg; 100 mg/kg
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Administration:p.o.; daily; 28 days
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Result:Significantly improved the 28-day survival rate in a dose-dependent manner.
Demonstrated sufficient tolerance at all tested doses (10 to 100 mg/kg).
Chemical Information
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CAS No. 1613437-67-4
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Molecular Weight 575.05
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Formula C31H31ClN4O5
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SMILES
O=C(C1=CC(NC/2=O)=C(C=C1)C2=C(NC3=CC4=C(N(C(CN5CCOCC5)=O)CC4)C=C3)/C6=CC=CC=C6)OC.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Huang Z, et al. Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis. ACS medicinal chemistry letters. 2017 Nov 09;8(11):1142-1147. [Content Brief]
[2]. Huang Z, et al. Characterization of preclinical in vitro and in vivo pharmacokinetics properties for KBP-7018, a new tyrosine kinase inhibitor candidate for treatment of idiopathic pulmonary fibrosis. Drug design, development and therapy. 2015;9:4319-28. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
KBP-7018 hydrochloride Related Classifications
HY-117873A Related Classifications
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