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| | DDR1-IN-2 Basic information | | Uses |
| Product Name: | DDR1-IN-2 | | Synonyms: | 4-Ethyl-N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)-3-(pyrazolo[1,5-a]pyrimidin-6-ylethynyl)benzamide;4-ETHYL-N-{3-[(4-METHYLPIPERAZIN-1-YL)METHYL]-5-(TRIFLUOROMETHYL)PHENYL-3-(2-{PYRAZOLO[1,5-A]PYRIMIDIN-6-YLETHYNYL)BENZAMIDE;DDR1-IN-2;DDR1 Inhibitor 7rh;Benzamide, 4-ethyl-N-[3-[(4-methyl-1-piperazinyl)methyl]-5-(trifluoromethyl)phenyl]-3-(2-pyrazolo[1,5-a]pyrimidin-6-ylethynyl)-;DDR1 Inhibitor 7rh >=98% (HPLC);7rh;DDR1 IN 2,Discoidin Domain Receptor,Inhibitor,7rh,inhibit,DDR-1-IN-2,DDR1IN2 | | CAS: | 1429617-90-2 | | MF: | C30H29F3N6O | | MW: | 546.59 | | EINECS: | | | Product Categories: | | | Mol File: | 1429617-90-2.mol |  |
| | DDR1-IN-2 Chemical Properties |
| storage temp. | 2-8°C | | solubility | DMSO: 62.5 mg/mL (114.35 mM) | | form | powder | | color | white to beige |
| | DDR1-IN-2 Usage And Synthesis |
| Uses | 7rh is a useful research chemical compound. | | Uses | 7rh is a discoidin domain receptor 1 (DDR1) inhibitor useful in the study of similar derivatives as potential anticancer and anti-??inflammatory drugs. | | General Description | DDR1 Inhibitor 7rh is a small potent kinase inhibitor of discoidin domain receptor-1 (DDR1). It inhibits the tumorigenicity of nasopharyngeal carcinoma (NPC) cells. DDR1 Inhibitor 7rh prevents the proliferation, invasion and adhesion of cancer cells. | | Biochem/physiol Actions | DDR1 Inhibitor 7rh is an orally available, potent, ATP-competitive DDR1-selective inhibitor with in vitro and in vivo anti-cancer efficacy. Compound 7rh is a potent, high affinity (Kd =0.6 nM), ATP-competitive inhibitor against discoidin domain-containing receptor 1 (DDR1; IC50 = 6.8 nM, [ATP] = 100 nM) with significantly reduced potency toward 455 other kinases, including DDR2, Bcr-abl, and c-Kit (IC50 = 101.4 nM, 355 nM and >10 μM, respectively). Inhibitor 7rh reduces DDR1 expression/phosphorylation and downstream signaling in a dose-dependent manner (0.1-2 μM; NCI-H23 NSCLCs), effectively suppressing human cancer cells proliferation (IC50 from 38 nM/K562 to 2.98 μM/NCI-H460) and colony formation (IC50 = 0.56 μM/NCI-H23). Inhibitor 7rh is orally availabe in rats and mice (T1/2 = 15.53 h; Tmax = 4.25 h; Cmax = 1867.5 μg/L, F = 67.4%; 25 mg/kg; rats) and displays in vivo efficacy against Kras (LSLG12Vgeo) tumor growth in mice (50 mg/kg/day p.o.). | | storage | Store at -20°C |
| | DDR1-IN-2 Preparation Products And Raw materials |
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