CAS 143851-98-3|Elacridar hydrochloride

Introduction：Basic information about CAS 143851-98-3|Elacridar hydrochloride, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Elacridar hydrochloride BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Customs
6. Synonyms

Common Name	Elacridar hydrochloride
CAS Number	143851-98-3	Molecular Weight	600.10400
Density	/	Boiling Point	701.6ºC at 760 mmHg
Molecular Formula	C₃₄H₃₄ClN₃O₅	Melting Point	/
MSDS	/	Flash Point	378.1ºC

Names

Name	N-[4-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]phenyl]-5-methoxy-9-oxo-10H-acridine-4-carboxamide,hydrochloride
Synonym	More Synonyms

Elacridar hydrochloride BiologicalActivity

Description	Elacridar Hcl (GF120918; GW0918) is a P-glycoprotein inhibitor, and has been used both in vitro and in vivo as a tool inhibitor of P-glycoprotein (Pgp) to investigate the role of transporters in the disposition of various test molecules.IC50 value:Target: P-glycoprotein In vitro, GF120918A demonstrated high plasma protein binding across species, although a definitive protein binding evaluation was precluded by poor recovery, particularly in buffer and in mouse, rat, and dog plasma. GF120918A did not demonstrate potent inhibition of several human cytochrome P450 enzymes evaluated in vitro, with IC(50) values well above concentrations anticipated to be achieved in vivo. Together, these data confirm the utility of GF120918A as a tool P-glycoprotein inhibitor in preclinical species and offer additional guidance on preclinical dose regimens likely to produce P-glycoprotein-mediated effects.
Related Catalog	Signaling Pathways >>Membrane Transporter/Ion Channel >>P-glycoproteinResearch Areas >>Cancer
References	[1]. Sane R, Mittapalli RK, Elmquist WF. Development and evaluation of a novel microemulsion formulation of elacridar to improve its bioavailability. J Pharm Sci. 2013 Jan 18. [2]. Bankstahl JP, Bankstahl M, Romermann K, et al. Tariquidar and Elacridar Are Dose-Dependently Transported by P-Glycoprotein and Bcrp at the Blood-Brain Barrier: A Small-Animal PET and In-Vitro Study. Drug Metab Dispos. 2013 Jan 10. [3]. Sane R, Agarwal S, Elmquist WF. Brain distribution and bioavailability of elacridar after different routes of administration in the mouse. Drug Metab Dispos. 2012 Aug;40(8):1612-9. [4]. Tang SC, Lagas JS, Lankheet NA, et al. Brain accumulation of sunitinib is restricted by P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) and can be enhanced by oral elacridar and sunitinib coadministration. Int J Cancer. 2012 Jan 1;130(1):223-33. doi: 10.1002/ijc.26000. [5]. Kuppens IE, Witteveen EO, Jewell RC, et al. A phase I, randomized, open-label, parallel-cohort, dose-finding study of elacridar (GF120918) and oral topotecan in cancer patients. Clin Cancer Res. 2007 Jun 1;13(11):3276-85. [6]. Hong Xiao, et al. Polymeric nanovesicle as simultaneous delivery platform with Doxorubicin conjugation and Elacridar encapsulation for enhanced treatment of multidrug-resistant breast cancer. J. Mater. Chem. B. 2018 Oct.

Description

Elacridar Hcl (GF120918; GW0918) is a P-glycoprotein inhibitor, and has been used both in vitro and in vivo as a tool inhibitor of P-glycoprotein (Pgp) to investigate the role of transporters in the disposition of various test molecules.IC50 value:Target: P-glycoprotein In vitro, GF120918A demonstrated high plasma protein binding across species, although a definitive protein binding evaluation was precluded by poor recovery, particularly in buffer and in mouse, rat, and dog plasma. GF120918A did not demonstrate potent inhibition of several human cytochrome P450 enzymes evaluated in vitro, with IC(50) values well above concentrations anticipated to be achieved in vivo. Together, these data confirm the utility of GF120918A as a tool P-glycoprotein inhibitor in preclinical species and offer additional guidance on preclinical dose regimens likely to produce P-glycoprotein-mediated effects.

Related Catalog

Signaling Pathways >>Membrane Transporter/Ion Channel >>P-glycoproteinResearch Areas >>Cancer

References

[1]. Sane R, Mittapalli RK, Elmquist WF. Development and evaluation of a novel microemulsion formulation of elacridar to improve its bioavailability. J Pharm Sci. 2013 Jan 18.

[2]. Bankstahl JP, Bankstahl M, Romermann K, et al. Tariquidar and Elacridar Are Dose-Dependently Transported by P-Glycoprotein and Bcrp at the Blood-Brain Barrier: A Small-Animal PET and In-Vitro Study. Drug Metab Dispos. 2013 Jan 10.

[3]. Sane R, Agarwal S, Elmquist WF. Brain distribution and bioavailability of elacridar after different routes of administration in the mouse. Drug Metab Dispos. 2012 Aug;40(8):1612-9.

[4]. Tang SC, Lagas JS, Lankheet NA, et al. Brain accumulation of sunitinib is restricted by P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) and can be enhanced by oral elacridar and sunitinib coadministration. Int J Cancer. 2012 Jan 1;130(1):223-33. doi: 10.1002/ijc.26000.

[5]. Kuppens IE, Witteveen EO, Jewell RC, et al. A phase I, randomized, open-label, parallel-cohort, dose-finding study of elacridar (GF120918) and oral topotecan in cancer patients. Clin Cancer Res. 2007 Jun 1;13(11):3276-85.

[6]. Hong Xiao, et al. Polymeric nanovesicle as simultaneous delivery platform with Doxorubicin conjugation and Elacridar encapsulation for enhanced treatment of multidrug-resistant breast cancer. J. Mater. Chem. B. 2018 Oct.

Chemical & Physical Properties

Boiling Point	701.6ºC at 760 mmHg
Molecular Formula	C₃₄H₃₄ClN₃O₅
Molecular Weight	600.10400
Flash Point	378.1ºC
Exact Mass	599.21900
PSA	92.89000
LogP	6.37310
Vapour Pressure	1.57E-19mmHg at 25°C
InChIKey	IQOJZZHRYSSFJM-UHFFFAOYSA-N
SMILES	COc1cc2c(cc1OC)CN(CCc1ccc(NC(=O)c3cccc4c(=O)c5cccc(OC)c5[nH]c34)cc1)CC2.Cl
Storage condition	2-8℃

Safety Information

HS Code	2934999090

Customs

HS Code	2934999090
Summary	2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Synonyms

UNII-NX2BHH1A5B

Elacridar HCl

Elacridar hydrochloride

Elacridar hydrochloride (USAN)

Elacridar (hydrochloride)

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