PF-06840003


Catalog No. Size PriceQuantity
M18659-2 2 mg solid $45
M18659-10 10 mg solid $80
M18659-C Contact sales@xcessbio.com for quotation $100

Description

PF-06840003 (EOS200271) is a highly selective orally bioavailable IDO-1 inhibitor with IC50s of 0.41 μM, 0.59 μM, and 1.5 μM for hIDO-1, dIDO-1, and mIDO-1, respectively.

Product information

CAS Number: 198474-05-4

Molecular Weight: 232.21

Formula: C12H9FN2O2

Chemical Name: 3-(5-fluoro-1H-indol-3-yl)pyrrolidine-2,5-dione

Smiles: O=C1NC(=O)CC1C1=CNC2C=CC(F)=CC1=2

InChiKey: MXKLDYKORJEOPR-UHFFFAOYSA-N

InChi: InChI=1S/C12H9FN2O2/c13-6-1-2-10-7(3-6)9(5-14-10)8-4-11(16)15-12(8)17/h1-3,5,8,14H,4H2,(H,15,16,17)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : ≥ 100 mg/mL (430.64 mM).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

PF-06840003 reverses IDO-1-induced T-cell anergy in vitro. PF-06840003 shows activity both in the HeLa assay (IC50=1.8 μM) as well as in the LPS/ INFγ-stimulated THP1 cells (IC50=1.7 μM).

In Vivo:

PF-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.

Products are for research use only. Not for human use.

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