PD-166866

Details

Stereochemistry	ACHIRAL
Molecular Formula	C20H24N6O3
Molecular Weight	396.443
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

COC1=CC(=CC(OC)=C1)C2=CC3=CN=C(N)N=C3N=C2NC(=O)NC(C)(C)C

InChI

InChIKey=NHJSWORVNIOXIT-UHFFFAOYSA-N

InChI=1S/C20H24N6O3/c1-20(2,3)26-19(27)25-17-15(8-12-10-22-18(21)24-16(12)23-17)11-6-13(28-4)9-14(7-11)29-5/h6-10H,1-5H3,(H4,21,22,23,24,25,26,27)

HIDE SMILES / InChI

Molecular Formula	C20H24N6O3
Molecular Weight	396.443
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/17987803 | https://www.ncbi.nlm.nih.gov/pubmed/9655904 | https://www.ncbi.nlm.nih.gov/pubmed/26993162

PD-166866 is a member of a new structural class of tyrosine kinase inhibitors, the 6-aryl-pyrido[2,3-d]pyrimidines. PD 166866 is an inhibitor of FGFR1. PD166866 might be used in the control of fibrotic proliferative diseases, as well as in other tumor pathologies. PD166866 inhibits proliferation and triggers anoikis in FGFR1-amplified breast cancer cell lines. Mechanistic study reveals that PD166866 induces autophagy through repressing Akt/mTOR signaling pathway.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Fibroblast growth factor receptor 1 46 Target ID: CHEMBL3650 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9655904	Inhibitor 8504		52.4 nM [IC50]
Akt/mTOR signaling pathway 1 Target ID: Akt/mTOR signaling pathway Sources: https://www.ncbi.nlm.nih.gov/pubmed/26993162	Inhibitor 8504

Conditions

Condition	Modality	Highest Phase	Product
Breast cancer 432 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26993162	Primary	Basic research	Unknown Approved Use Unknown
Sarcoma 14 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24719266 https://www.ncbi.nlm.nih.gov/pubmed/15814652	Primary	Basic research	Unknown Approved Use Unknown
Cancer 609 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20003343 https://www.ncbi.nlm.nih.gov/pubmed/17987803	Primary	Basic research	Unknown Approved Use Unknown

PubMed

Title	Date	PubMed
Increased glutathione biosynthesis by Nrf2 activation in astrocytes prevents p75NTR-dependent motor neuron apoptosis.	2006-05	16524372
Astrocyte activation by fibroblast growth factor-1 and motor neuron apoptosis: implications for amyotrophic lateral sclerosis.	2005-04	15773903
Essential role of fibroblast growth factor signaling in preadipoctye differentiation.	2005-02	15522930
Hypoxia-responsive growth factors upregulate periostin and osteopontin expression via distinct signaling pathways in rat pulmonary arterial smooth muscle cells.	2004-10	15121739
Thyroid hormone activates fibroblast growth factor receptor-1 in bone.	2003-09	12805413

Patents

Sample Use Guides

In Vivo Use Guide

Unknown

Route of Administration: Unknown

In Vitro Use Guide

L6 cells overexpressing FGF receptors were treated for 8 consecutive days with concentrations of PD-166866 from 1 to 100 nM. L6 cells exposed to bFGF alone (25 ng/ml) elicit a pronounced growth response in culture. The addition of PD 166866 together with bFGF produced a potent, concentration-related inhibition of bFGF-stimulated cell growth with an IC50 value of 24.1 nM (n = 3) by the eighth day. At a concentration of 100 nM PD 166866, bFGF-driven growth of L6 cells was almost suspended.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 22:45:24 GMT 2025` Edited by `admin` on `Mon Mar 31 22:45:24 GMT 2025`
Record UNII	NA856793UT
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

PD-166866

Common Name

English

1-(2-AMINO-6-(3,5-DIMETHOXYPHENYL)-PYRIDO(2,3-D)PYRIMIDIN-7-YL)-3-TERT-BUTYL UREA

Preferred Name

English

UREA, N-(2-AMINO-6-(3,5-DIMETHOXYPHENYL)PYRIDO(2,3-D)PYRIMIDIN-7-YL)-N'-(1,1-DIMETHYLETHYL)-

Systematic Name

English

Code System Code Type Description

PUBCHEM

5328127