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PF-06840003
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。
PF-06840003图片
CAS NO:198474-05-4
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 232.21
Formula C12H9FN2O2
CAS No. 198474-05-4
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: ≥ 28 mg/mL
Water:
Ethanol:
Chemical Name 3-(5-Fluoro-1H-indol-3-yl)pyrrolidine-2,5-dione
Synonyms PF-06840003; PF 06840003; PF06840003; EOS200271, EOS-200271; EOS 200271
SMILES Code O=C(C(C1=CNC2=C1C=C(F)C=C2)C3)NC3=O
实验参考方法
In Vitro

In vitro activity: PF-06840003 (also known as EOS200271) is a highly potent and selective, orally bioavailable IDO-1 inhibitor with IC50 of 0.15 μM. It is a tryptophan analog, noncompetitive, and non-heme-binding IDO1 inhibitor licensed by iTeos SA to Pfizer for clinical development. Tumors use tryptophan-catabolizing enzymes such as indoleamine 2,3-dioxygenase (IDO-1) to induce an immunosuppressive environment. IDO-1 is induced in response to inflammatory stimuli and promotes immune tolerance through effector T-cell anergy and enhanced Treg function. As such, IDO-1 is a nexus for the induction of a key immunosuppressive mechanism and represents an important immunotherapeutic target in oncology. PF-06840003 has favorable human pharmacokinetic characteristics, a prolonged human half-life that may allow single-dose daily administration, and CNS penetration


Kinase Assay: . PF-0684000 has moderate hIDO1 enzyme inhibition with IC50 0.41 μM. It is a highly efficient compound which is driven by its tight packing within the enzyme, as well as the high density of hydrogen bonds it forms with hIDO-1 despite its small size.


Cell Assay:

In VivoPF-06840003 reduces intratumoral kynurenine levels in mice by>80% and inhibits tumor growth in multiple preclinical syngeneic models in mice, in combination with immune checkpoint inhibitors. PF-0684003 has favorable predicted human pharmacokinetic properties, including a predicted t1/2 of 16-19 hours.
Animal model Mice
Formulation & Dosage p.o.
References AACR; Cancer Res 2016;76(14 Suppl):Abstract nr4863.