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首页-小分子抑制剂&激动剂-Tyrosine Kinase-FGFR-Pemigatinib
Pemigatinib

Chemical Structure : Pemigatinib

CAS No.: 1513857-77-6

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Pemigatinib (INCB054828;INCB 054828)

货号: PC-61394Not For Human Use, Lab Use Only.

Pemigatinib (INCB054828, INCB 054828) is a potent, selective, orally bioavailable inhibitor of FGFR1/2/3 with IC50 of 0.4 nM, 0.5 nM, 1.2 nM and 30 nM for FGFR1/2/3/4, respectively.

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10 mg ￥1480 In stock
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50 mg ￥3980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Pemigatinib (INCB054828, INCB 054828) is a potent, selective, orally bioavailable inhibitor of FGFR1/2/3 with IC50 of 0.4 nM, 0.5 nM, 1.2 nM and 30 nM for FGFR1/2/3/4, respectively.
Pemigatinib (INCB054828) potently inhibits the kinase activity of recombinant FGFR1, FGFR2 and FGFR3 enzymes and is highly selective against a panel of kinases including VEGFR2.
Pemigatinib (INCB054828) inhibits the autophosphorylation of FGFR proteins with low nanomolar IC50 values and blocks signal transduction by FGFR to downstream markers of pathway activation.
Cancer cell lines that have genetic alterations in FGFR1, FGFR2 and FGFR3 were uniquely displays sensitivity to cancer cell growth that have genetic alterations in FGFR1, FGFR2 and FGFR3 with IC50 in the range of 3-50 nM, with little to no effect on cancer cell lines or normal cells without FGFR dependence (IC50>1.5 uM).
Pemigatinib (INCB054828) inhibits the growth of tumors that are dependent upon FGFR1, FGFR2 and FGFR3 activity in vivo, which is dose-dependent and correlated with pharmacodynamic inhibition of FGFR.

物理化学性质&存储条件

分子量 487.5
分子式 C24H27F2N5O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-ethyl-8-[(morpholin-4-yl)methyl]-1,3,4,7-tetrahydro-2Hpyrrolo[3',2':5,6]pyrido[4,3-d]pyrimidin-2-one

参考文献

1. Phillip CC Liu, et al. Abstract 771: Preclinical characterization of the selective FGFR inhibitor INCB054828. AACR DOI: 10.1158/1538-7445.AM2015-771 Published August 2015.
2. Mansoor Saleh, et al. Abstract CT111: Preliminary results from a phase 1/2 study of INCB054828, a highly selective fibroblast growth factor receptor (FGFR) inhibitor, in patients with advanced malignancies. AACR DOI: 10.1158/1538-7445.AM2017-CT111 Published July 2017.

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