MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Infigratinib phosphate

CAS No. : 1310746-10-1

MCE 站：Infigratinib phosphate

产品活性：Infigratinib phosphate (BGJ-398 phosphate; NVP-BGJ398 phosphate) 是 FGFR 抑制剂，对 FGFR1，FGFR2 和 FGFR3 的 IC₅₀ 分别为0.9，1.4 和 1 nM，比对 FGFR4 和 VEGFR2 的抑制性高40倍，对 Abl，Fyn，Kit，Lck 和 Lyn几乎无活性。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：FGFR

In Vitro: Infigratinib phosphate inhibits FGFR1, FGFR2, ａnd FGFR3 with IC₅₀=~1 nM, FGFR3^K650E with IC₅₀=4.9 nM, ａnd FGFR4 with IC₅₀=60 nM. IC₅₀ values for all other kinases are in the μM range (FYN, LCK, YES, ａnd ABL, IC₅₀=1.9, 2.5, 1.1, ａnd 2.3 μM, respectively) except for VEGFR2, KIT, ａnd LYN, which are inhibited at submicromolar concentrations (IC₅₀=0.18, 0.75, ａnd 0.3 μM, respectively). Infigratinib inhibits the proliferation of the FGFR1-, FGFR2-, ａnd FGFR3-dependent BaF3 cells with IC₅₀ values which are in the low nanomolar range ａnd comparable to those observed for the inhibition of the receptors kinase activity in the enzymatic assay. For the remaining cells, all IC₅₀ values are greater than 1.5 μM except for VEGFR2 (IC₅₀ 1449 ａnd 938 nM), for which there is at least a 400-fold selectivity versus FGFR1, FGFR2, ａnd FGFR3. Infigratinib (ranging between 1 nM ａnd 10 μM) is potent at inhibiting cell growth of FGFR2-mutant endometrial cancer cells.

In Vivo: Infigratinib is administered to athymic nude mice implanted subcutaneously with RT112/luc1 tumors: either as a 5 mg/kg intravenous bolus in NMP/PEG200 (1:9, v/v) or orally by gavage as a suspension in PEG300/D5W (2:1, v/v) at a 20 mg/kg dose. The relevant pharmacokinetic (PK) parameters indicate that the oral bioavailability of Infigratinib in this study is 32%. After intravenous dosing, Infigratinib shows a rapid distribution from the vascular compartment into the peripheral tissues, translating into a high volume of distribution (26 L/kg). The plasma clearance is high at 3.3 L/h/kg (61% of liver blood flow). The ratio of tumor to plasma after oral dosing based on AUC is determined to be 10. Infigratinib (30 mg/kg) significantly inhibits the growth of FGFR2-mutated endometrial cancer xenograft models.

相关产品：SU 5402  |  Heparan Sulfate  |  PD173074  |  Formotin  |  Gandotinib  |  KW-2449  |  Ferulic acid  |  PD-166866  |  CP-547632  |  PP58  |  SUN11602  |  R1530  |  2,5-Dihydroxybenzoic acid  |  Tyrosine kinase-IN-1  |  PD-161570  |  ARQ 069  |  PD-089828  |  SM1-71  |  SU4984

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。