Infigratinib (BGJ-398; NVP-BGJ398) is a potent inhibitor of theFGFRfamily withIC₅₀s of 0.9 nM, 1.4 nM, 1 nM, and 60 nM forFGFR1,FGFR2,FGFR3, andFGFR4, respectively.

Infigratinib (BGJ-398) inhibits FGFR1, FGFR2, and FGFR3 with IC₅₀=~1 nM, FGFR3^K650Ewith 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 (BGJ-398) 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 (BGJ-398) (ranging between 1 nM and 10 μM) is potent at inhibiting cell growth ofFGFR2-mutant endometrial cancer cells^[2].

Infigratinib (BGJ-398) 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 (BGJ-398) in this study is 32%. After intravenous dosing, Infigratinib (BGJ-398) 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 (BGJ-398) (30 mg/kg) significantly inhibits the growth ofFGFR2-mutated endometrial cancer xenograft models^[2].

560.48

Solid

C₂₆H₃₁Cl₂N₇O₃

872511-34-7

Room temperature in continental US; may vary elsewhere.

DMSO : 12 mg/mL(21.41 mM;Need ultrasonic)

H₂O :< 0.1 mg/mL(insoluble)

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。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    90% (20%SBE-β-CDin saline)

  Solubility: 1.67 mg/mL (2.98 mM); Suspended solution; Need ultrasonic

  此方案可获得 1.67 mg/mL (2.98 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

  以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 2.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 1.67 mg/mL (2.98 mM); Clear solution

  此方案可获得 ≥ 1.67 mg/mL (2.98 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• 3.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

  Solubility: ≥ 1.57 mg/mL (2.80 mM); Clear solution

  此方案可获得 ≥ 1.57 mg/mL (2.80 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 15.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 4.

  请依序添加每种溶剂： 5% DMSO    40%PEG300   5%Tween-80   50% saline

  Solubility: ≥ 0.6 mg/mL (1.07 mM); Clear solution
• 5.

  请依序添加每种溶剂： 5% DMSO    95% (20%SBE-β-CDin saline)

  Solubility: ≥ 0.6 mg/mL (1.07 mM); Clear solution