FGFR-IN-13

CAS: 2962941-25-7 F: C23H21N5O3 W: 415.44

FGFR-IN-13 (compound III-30) is an irreversible covalent fibroblast growth factor receptor (FGFR) inhibitor. FGFR-IN-13

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Bioactivity	FGFR-IN-13 (compound III-30) is an irreversible covalent fibroblast growth factor receptor (FGFR) inhibitor. FGFR-IN-13 regulates endogenous FGFR1(IC50=0.20±0.02 nM) and FGFR4(IC50=0.40±0.03 nM) mediated signaling pathways by inhibiting the expression of key proteins. FGFR-IN-13 inhibits total-PARP and Bcl-2 protein expressions, and promote Cleaved-PARP and Bax protein expressions in a dose-dependent manner. FGFR-IN-13 has significant antitumor activity and oral activity[1].
Invitro	FGFR-IN-13 (10 μM, 9 h) 可以和 FGFR 蛋白实现共价不可逆结合，其抑制 p-FGFR 蛋白表达的能力可以达到 AZD4547(HY-13330) 和 TAS-120(HY-100818) 的水平在 MDA-MB-231 细胞系中[1]。FGFR-IN-13 (2.5, 5, 10 μM, 24 h) 能呈剂量依赖性诱导细胞凋亡，在相同浓度 (5 μM) 下诱导凋亡能力优于AZD4547 (45.4% 和 37.3%)，可能具有与 AZD4547 相似的作用机制，但 MDAMB-231 细胞对 III-30 更为敏感[1]。FGFR-IN-13 (1.25, 2.5, 5 μM, 12 h) 在不产生明显细胞毒性的剂量下，能有效抑制MDA-MB-231细胞的迁移，且呈剂量依赖性[1]。FGFR-IN-13 (2.5, 5, 10 μM, 12 h) 能够通过产生过量的ROS和降低MMP来诱导细胞凋亡[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> FGFR-IN-13 相关抗体: Western Blot Analysis[1] Cell Line:
In Vivo	FGFR-IN-13 (10 和 30 mg/kg，每天口服一次持续 21 天) 抑制肿瘤生长呈剂量依赖性，且具有良好的安全性，在安全剂量下可有效抑制肿瘤生长在 MDA-MB-231 异种移植瘤小鼠模型[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
CAS	2962941-25-7
Formula	C23H21N5O3
Molar Mass	415.44
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Wang Y, et al. Discovery of N-(4-((6-(3, 5-Dimethoxyphenyl)-9H-Purine Derivatives as Irreversible Covalent FGFR Inhibitors[J]. European Journal of Medicinal Chemistry, 2024: 116415.

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