Infigratinib phosphate
作者：齊岳
發布時間：2023-08-25
08:58:40
點擊數：
產品名稱：Infigratinib phosphate
產品描述：
| 產品描述 | Infigratinib phosphate is an effective inhibitor of the FGFR family (IC50: 0.9 nM, 1.4 nM, 1 nM, and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively). |
| 靶點活性 | FGFR1:0.9 nM, FGFR2:1.4 nM, FGFR3:1 nM, FGFR4:60 nM |
| 體外活性 | 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. Infigratinib phosphate suppresses FGFR1, FGFR2, and FGFR3(IC50=~1 nM), FGFR3K650E(IC50=4.9 nM), and FGFR4(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 (ranging between 1 nM and 10 μM) is effective at inhibiting cell growth of FGFR2-mutant endometrial cancer cells. 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[1][2]. |
| 體內活性 | Infigratinib (30 mg/kg) significantly suppresses the growth of FGFR2-mutated endometrial cancer xenograft models. 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.Infigratinib shows a rapid distribution from the vascular compartment into the peripheral tissues after intravenous dosing, translating into a high volume of distribution (26 L/kg). The relevant pharmacokinetic (PK) parameters indicate that the oral bioavailability of Infigratinib in this study is 32%. 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 [1][2]. |
| 別名 | BGJ-398 phosphate, NVP-BGJ398 phosphate |
| 分子量 | 658.47 |
| 分子式 | C26H34Cl2N7O7P |
| CAS No. | 1310746-10-1 |
存儲
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 11.7mg/mL (17.8mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
聯系我們：
郵箱：2519696869@qq.com
QQ: 2519696869
電話：18066853083
微信：18066853083
公司介紹：
西安齊岳生物科技有限公司是集化學科研和定制與一體的高科技化學公司。業務范圍包括化學試劑和產品的研發、生產、銷售等。涉及產品為通用試劑的分銷、非通用試劑的定制與研發，涵蓋生物科技、化學品、中間體和化工材料等領域。
主營產品：COF、MOF單體系列：三蝶烯衍生物、金剛烷衍生物、四苯甲烷衍生物、peg、上轉換、石墨烯、光電材料、點擊化學、凝集素、載玻片、蛋白質交聯劑、脂質體、蛋白、多肽、氨基酸、糖化學等。
