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Details

Stereochemistry ACHIRAL
Molecular Formula C30H26F2N4O5
Molecular Weight 560.548
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of N-[4-(6,7-dimethoxyquinolin-4-yl)oxy-3-fluorophenyl]-4-ethoxy-1-(4-fluoro-2-methylphenyl)pyrazole-3-carboxamide

SMILES

CCOC1=CN(N=C1C(=O)NC2=CC=C(OC3=C4C=C(OC)C(OC)=CC4=NC=C3)C(F)=C2)C5=CC=C(F)C=C5C

InChI

InChIKey=ISPBCAXOSOLFME-UHFFFAOYSA-N
InChI=1S/C30H26F2N4O5/c1-5-40-28-16-36(23-8-6-18(31)12-17(23)2)35-29(28)30(37)34-19-7-9-25(21(32)13-19)41-24-10-11-33-22-15-27(39-4)26(38-3)14-20(22)24/h6-16H,5H2,1-4H3,(H,34,37)

HIDE SMILES / InChI

Molecular Formula C30H26F2N4O5
Molecular Weight 560.548
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

LDC1267 preferentially inhibits TAM tyrosine kinase receptors Tyro3, Axl and Mer at low nanomolarity. LDC1267 conferred therapeutic potential, efficiently enhancing anti-metastatic natural killer (NK) cells activity. In vivo the compound markedly reduced murine mammary cancer and melanoma metastases dependent on NK cells.

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
8.0 nM [IC50]
5.0 nM [IC50]
29.0 nM [IC50]
35.0 nM [IC50]
36.0 nM [IC50]
51.0 nM [IC50]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown
Primary
Unknown

PubMed

Sample Use Guides

In Vivo Use Guide
Mice treated intraperitoneally with LDC1267 (20 mg/kg) or by oral gavage LDC1267 (100 mg/kg).
Route of Administration: Other
In Vitro Use Guide
LDC1267 (up to 30 mM) did not affect proliferation of 84 cell lines and moderately affected proliferation of 11 cell lines (best IC50 value at ,5 mM; average IC50 value for those 11 cell lines is ,15 mM).
Substance Class Chemical
Record UNII
DK8ACB2D8P
Record Status Validated (UNII)
Record Version