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Elacridar

Elacridar structure

CAS No:
143664-11-3
Formula:
C34H33N3O5
Chemical Name:
Elacridar
Synonyms:
4-Acridinecarboxamide,N-[4-[2-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-9,10-dihydro-5-methoxy-9-oxo-;N-[4-[2-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-9,10-dihydro-5-methoxy-9-oxo-4-acridinecarboxamide;GF 120918;GG 918;Elacridar;GW 0918;GF 129018
Categories:
Biochemical Engineering > Inhibitors

Description

Yellow Solid

Elacridar (GW120918) is an oral bioenhancer that targets multiple drug resistance in tumors. In many cases, the appearance of multidrug resistance in cancer is due to a change in expression of protein inhibitors. As of August 2007 elacridar was not listed on GSK's product pipeline. Development is assumed to have been discontinued.

Elacridar Basic Attributes

Molecular Weight：

563.64292

Exact Mass：

563.64

UNII：

N488540F94

DSSTox ID：

DTXSID90162489

HScode：

29334900

Characteristics

PSA：

89.1

XLogP3：

5.6

Appearance：

white to beige

Density：

1.264±0.06 g/cm3(Predicted)

Melting Point：

216-218°C

Boiling Point：

701.6±60.0 °C(Predicted)

Flash Point：

378.1±32.9 °C

Refractive Index：

1.644

Water Solubility：

DMSO: soluble2mg/mL (clear solution, warmed)

Storage Conditions：

-20°C Freezer

Safety Information

Transport codes：

NONH for all modes of transport

wgk germany：

safety instructions：

24/25

RTECS Number：

AR7621300

Drug Information

Drug Indication：

For the treatment of solid tumors.

Pharmacology：

Elacridar is an oral bioenhancer that targets multiple drug resistance in tumors. In many cases, the appearance of multidrug resistance in cancer is due to a change in expression of protein inhibitors.

Mechanism of Action：

P-glycoprotein is a well characterized human ABC-transporter of the MDR/TAP subfamily. It is an ATP-dependent efflux pump with broad substrate specificity. It likely evolved as a defence mechanism against harmful substances. Increased intestinal expression of P-glycoprotein can reduce the absorption of drugs that are substrates for P-glycoprotein. Thus, there is a reduced bioavailability, therapeutic plasma concentrations are not attained. Elacridar functions by inhibiting P-glycoprotein, resulting in an increased bioavailability of coadminstered drugs.

MeSH Entry Terms：

Elacridar

Elacridar Use and Manufacturing

A prototypical BCRP inhibitor. Inhibits the Bcrp1-mediated transport.

Computed Properties

Molecular Weight:563.6
XLogP3:5.6
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:7
Rotatable Bond Count:8
Exact Mass:563.24202116
Monoisotopic Mass:563.24202116
Topological Polar Surface Area:89.1
Heavy Atom Count:42
Complexity:925
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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Elacridar

CAS No.: 143664-11-3

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