FGFR1/DDR2 inhibitor 1

未知

FGFR1/DDR2 抑制剂 1

FGFR1/DDR2 inhibitor 1

F656871-1ml

1ml

10mM in DMSO

-80℃储存

超低温冰袋运输

FGFR1/DDR2 inhibitor 1 is an orally active inhibitor of fibroblast growth factor receptor 1 (FGFR1) and discoindin domain receptor 2 (DDR2) , with IC 50 values of 31.1 nM and 3.2 nM, respectively. Antitumor activity In Vitro FGFR1/DDR2 inhibitor 1 (compound 11k) (25-200 μM; 2 hours) shows significant inhibition of FGFR2 phosphorylation in a dose-dependent manner in SNU16 cells. FGFR1/DDR2 inhibitor 1 shows (60-250 μM; 2 hours) significant inhibition of DDR2 phosphorylation in a dose-dependent manner in H2286 cells. FGFR1/DDR2 inhibitor 1 significantly inhibits the proliferation of FGFR-driven cancer cell lines with IC 50 s of 108.4, 93.4, 31.8 and 306.6 nM against KG-1, SNU-16, NCI-H716 and UMUC14 respectively. FGFR1/DDR2 inhibitor 1 demonstrates substantially activity against the DDR2-driven cancer cell line NCI-H2286 (93.0 nM). MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo FGFR1/DDR2 inhibitor 1 (10-20 mg/kg; p.o.; once daily for 7 days) has profound anti-tumor efficacy in NCI-H1581 tumor model . SCID mice bearing NCI-H2286 tumors were randomized and treated with FGFR1/DDR2 inhibitor 1 at doses of 10 mg/kg for 10 consecutive days. FGFR1/DDR2 inhibitor 1 could suppress tumor growth with tumor growth inhibition rates (TGI) of 82.8% . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Nude mice bearing NCI-H1581 tumors Dosage: 10 or 20 mg/kg Administration: P.o.; once daily for 7 days Result: Suppressed tumor growth in a dose-dependent manner with tumor growth inhibition rates (TGI) of 59.7% and 98.1% at doses of 10 and 20 mg/kg, respectively. IC50& Target:FGFR1 31.1 nM (IC 50 ) DDR2 3.2 nM (IC 50 )

FGFR1/DDR2 抑制剂 1 是一种具有口服活性的成纤维细胞生长因子受体 1（FGFR1）和 Discoindin 结构域受体 2（DDR2）抑制剂，其 IC 50 值分别为 31.1 nM 和 3.2 nM。抗肿瘤活性。

2308497-58-5(DMSO)

C28H22F3N5O

501.5 g/mol

CC1=C(C=C(C=C1)C(=O)NC2=CC=CC(=C2)C(F)(F)F)C3=CC4=C(C=C3)C(=NN4)C5=CN(N=C5)C6CC6

酪氨酸激酶