Erdafitinib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Erdafitinib (JNJ-42756493) 是一种高效、选择性的 FGFR 家族小分子抑制剂。

Erdafitinib (JNJ-42756493) is a highly potent and selective, small-molecule inhibitor of FGFR family with IC50s of 1.2/2.5/3/5.7 nM for FGFR1/2/3/4; shows rapid uptake into the lysosomal compartment of cells in culture, which is associated with prolonged inhibition of FGFR signaling; orally active.Blood Cancer Phase 2 Clinical(In Vitro):Erdafitinib (JNJ-42756493) inhibits the tyrosine kinase activities of FGFR1-4 in time-resolved fluorescence assays with IC50 values of 1.2, 2.5, 3.0 and 5.7 nM, respectively. The closely related VEGFR2 kinase is less potently inhibited (30-fold less potent compared to FGFR1) by erdafitinib, with an IC50 value of 36.8 nM. Erdafitinib binds FGFR1, 3, 4, and 2 with Kd values of 0.24, 1.1, 1.4 and 2.2 nM, respectively. The Kd value for VEGFR2 is higher at 6.6 nM. Erdafitinib inhibits proliferation of FGFR1, 3, and 4 expressing cells with IC50 values of 22.1, 13.2, and 25nM, respectively.(In Vivo):In xenografts from human tumor cell lines or patient-derived tumor tissue with activating FGFR alterations, Erdafitinib administration results in potent and dose-dependent antitumor activity accompanied by pharmacodynamic modulation of phospho-FGFR and phospho-ERK in tumors.

Erdafitinib (JNJ-42756493) inhibits the tyrosine kinase activities of FGFR1-4 in time-resolved fluorescence assays with IC50 values of 1.2, 2.5, 3.0 and 5.7 nM, respectively. The closely related VEGFR2 kinase is less potently inhibited (30-fold less potent compared to FGFR1) by erdafitinib, with an IC50 value of 36.8 nM. Erdafitinib binds FGFR1, 3, 4, and 2 with Kd values of 0.24, 1.1, 1.4 and 2.2 nM, respectively. The Kd value for VEGFR2 is higher at 6.6 nM. Erdafitinib inhibits proliferation of FGFR1, 3, and 4 expressing cells with IC50 values of 22.1, 13.2, and 25nM, respectively.

In xenografts from human tumor cell lines or patient-derived tumor tissue with activating FGFR alterations, Erdafitinib administration results in potent and dose-dependent antitumor activity accompanied by pharmacodynamic modulation of phospho-FGFR and phospho-ERK in tumors.

JNJ-42756493

Angiogenesis

FGFR

FGFR1|FGFR2|FGFR3|FGFR4

Cancer

Blood cancer

1346242-81-6

446.5447

C25H30N6O2

>98% (HPLC)

DMSO: ≥ 33 mg/mL

CC(NCCN(C1=CC(OC)=CC(OC)=C1)C2=CC=C3N=CC(C4=CN(C)N=C4)=NC3=C2)C

1,2-Ethanediamine, N1-(3,5-dimethoxyphenyl)-N2-(1-methylethyl)-N1-[3-(1-methyl-1H-pyrazol-4-yl)-6-quinoxalinyl]-

(-20℃)

With Ice Pack

≥ 2 years