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DDR1 inhibitor 7rh
CAS No. 1429617-90-2
DDR1 inhibitor 7rh( —— )
Catalog No. M11812 CAS No. 1429617-90-2
DDR1 inhibitor 7rh is a potent, selective, ATP-competitive, orally available Discoidin domain receptor 1 (DDR1) inhibitor with IC50 of 6.8 nM in cell-free kinase assays.
Purity : >98% (HPLC)
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Size | Price / USD | Stock | Quantity |
5MG | 87 | In Stock |
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10MG | 158 | In Stock |
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25MG | 329 | In Stock |
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50MG | 501 | In Stock |
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100MG | 734 | In Stock |
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500MG | 1467 | In Stock |
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1G | Get Quote | In Stock |
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Biological Information
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Product NameDDR1 inhibitor 7rh
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NoteResearch use only, not for human use.
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Brief DescriptionDDR1 inhibitor 7rh is a potent, selective, ATP-competitive, orally available Discoidin domain receptor 1 (DDR1) inhibitor with IC50 of 6.8 nM in cell-free kinase assays.
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DescriptionDDR1 inhibitor 7rh is a potent, selective, ATP-competitive, orally available Discoidin domain receptor 1 (DDR1) inhibitor with IC50 of 6.8 nM in cell-free kinase assays; DDR1 inhibitor 7rh is significantly less potent in suppressing the kinase activities of DDR2 (IC50=101 nM), Bcr-Abl (IC50=355 nM), and c-Kit (IC50>10 uM); inhibits DDR1-mediated signaling induced by soluble collagen (50 μg/ml) in a concentration-dependent manner, inhibits activation of PYK2 and PEAK1, signaling proteins downstream of DDR1 in PANC-1 cells; induces significant decrease of total protein levels of DDR1 and Bcl-xL, causes a significant reduction in the level of MMP-2 in NSCLS cells; suppresses the growth of K562 human CML cells with IC50 of 38 nM, A549, NCI-H23 and NCI-H460 human NSCLC cells with IC50 of 2.7, 2.1 and 3.0 μM, respectively; abrogates collagen-induced DDR1 signaling in pancreatic tumor cells and consequently reduces colony formation and migration, exhibits striking efficacy in combination with chemotherapy in orthotopic xenografts and autochthonous pancreatic tumors.
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In Vitro7rh (compound 1) is a potent inhibitor of DDR1, with an IC50 of 13.1 nM, and less potently inhibits DDR2, with an IC50 of 203 nM. 7rh also shows inhibitory activities against Bcr-Abl and c-Kit, with IC50s of 414 and 2500 nM, respectively.
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In Vivo——
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Synonyms——
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PathwayTyrosine Kinase
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TargetDDR
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RecptorDDR1|DDR2
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Research Area——
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Indication——
Chemical Information
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CAS Number1429617-90-2
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Formula Weight546.598
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Molecular FormulaC30H29F3N6O
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Purity>98% (HPLC)
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SolubilityDMSO: 12 mg/mL (21.95 mM), 18.3 mM ( < 1 mg/ml refers to the product slightly soluble or insoluble )
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SMILESCCC1=C(C=C(C=C1)C(=O)NC2=CC(=CC(=C2)C(F)(F)F)CN3CCN(CC3)C)C#CC4=CN5C(=CC=N5)N=C4
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Chemical Name4-Ethyl-N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)-3-(pyrazolo[1,5-a]pyrimidin-6-ylethynyl)benzamide
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Aguilera KY, et al. Mol Cancer Ther. 2017 Nov;16(11):2473-2485.
2. Gao M, et al. J Med Chem. 2013 Apr 25;56(8):3281-95.
molnova catalog
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