おすすめの製品
品質水準
アッセイ
≥98% (HPLC)
フォーム
powder
色
white to beige
溶解性
DMSO: 10 mg/mL, clear
保管温度
2-8°C
SMILES記法
O=C(NC1=CC(C(F)(F)F)=CC(CN2CCN(C)CC2)=C1)C3=CC=C(CC)C(C#CC4=CN5C(N=C4)=CC=N5)=C3
InChI
1S/C30H29F3N6O/c1-3-23-6-7-25(16-24(23)5-4-21-18-34-28-8-9-35-39(28)20-21)29(40)36-27-15-22(14-26(17-27)30(31,32)33)19-38-12-10-37(2)11-13-38/h6-9,14-18,20H,3,10-13,19H2,1-2H3,(H,36,40)
InChI Key
DDLPXZXBWGJRGK-UHFFFAOYSA-N
詳細
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.
生物化学的／生理学的作用
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.).
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.).
DDR1 Inhibitor 7rh is an orally available, potent, ATP-competitive DDR1-selective inhibitor with in vitro and in vivo anti-cancer efficacy.
保管分類コード
11 - Combustible Solids
WGK
WGK 3
引火点(°F)
Not applicable
引火点(℃)
Not applicable
最新バージョンのいずれかを選択してください：
試験成績書（COA）
Lot/Batch Number
Mingshan Gao et al.
Journal of medicinal chemistry, 56(8), 3281-3295 (2013-03-26)
Discoidin domain receptor 1 (DDR1) is an emerging potential molecular target for new anticancer drug discovery. We have discovered a series of 3-(2-(pyrazolo[1,5-a]pyrimidin-6-yl) ethynyl)benzamides that are selective and orally bioavailable DDR1 inhibitors. The two most promising compounds (7rh and 7rj)
Chiara Ambrogio et al.
Nature medicine, 22(3), 270-277 (2016-02-09)
Patients with advanced Kirsten rat sarcoma viral oncogene homolog (KRAS)-mutant lung adenocarcinoma are currently treated with standard chemotherapy because of a lack of efficacious targeted therapies. We reasoned that the identification of mediators of Kras signaling in early mouse lung
Protein Analysis and Purification: Benchtop Techniques, 3598-3608 (2018)
Hoon Hur et al.
BMC cancer, 17(1), 87-87 (2017-02-02)
Discoidin domain receptor 1 (DDR1), a receptor tyrosine kinase that utilizes collagen as a ligand, is a key molecule in the progression of solid tumors as it regulates the interaction of cancer cells with the tumor stroma. However, the clinical
Antitumor activity of 7RH, a discoidin domain receptor 1 inhibitor, alone or in combination with dasatinib exhibits antitumor effects in nasopharyngeal carcinoma cells
Lu QP, et al.
Oncology Letters, 12(5), 3598-3608 (2016)
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