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Infigratinib phosphate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Infigratinib phosphate图片
CAS NO:1310746-10-1
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议

产品名称
BGJ-398 phosphate
NVP-BGJ398 phosphate
产品介绍
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。
生物活性

Infigratinib phosphate (BGJ-398 phosphate; NVP-BGJ398 phosphate) is a potent inhibitor of theFGFRfamily withIC50of 0.9 nM, 1.4 nM, 1 nM, and 60 nM forFGFR1,FGFR2,FGFR3, andFGFR4, respectively.

IC50& Target[1]

FGFR1

0.9 nM (IC50)

FGFR2

1.4 nM (IC50)

FGFR3

1 nM (IC50)

FGFR4

60 nM (IC50)

体外研究
(In Vitro)

Infigratinib phosphate inhibits FGFR1, FGFR2, and FGFR3 with IC50=~1 nM, FGFR3K650Ewith IC50=4.9 nM, and FGFR4 with IC50=60 nM. IC50values 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 IC50values 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 IC50values are greater than 1.5 μM except for VEGFR2 (IC501449 and 938 nM), for which there is at least a 400-fold selectivity versus FGFR1, FGFR2, and FGFR3[1]. Infigratinib (ranging between 1 nM and 10 μM) is potent at inhibiting cell growth ofFGFR2-mutant endometrial cancer cells[2].

体内研究
(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[1]. Infigratinib (30 mg/kg) significantly inhibits the growth ofFGFR2-mutated endometrial cancer xenograft models[2].

Clinical Trial
分子量

658.47

性状

Solid

Formula

C26H34Cl2N7O7P

CAS 号

1310746-10-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : ≥ 12.5 mg/mL(18.98 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.5187 mL7.5934 mL15.1867 mL
5 mM0.3037 mL1.5187 mL3.0373 mL
10 mM0.1519 mL0.7593 mL1.5187 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。