Zosuquidar

Modify Date: 2024-01-02 21:14:32

Zosuquidar structure	Common Name	Zosuquidar
	CAS Number	167354-41-8	Molecular Weight	527.604
	Density	1.4±0.1 g/cm3	Boiling Point	690.5±55.0 °C at 760 mmHg
	Molecular Formula	C₃₂H₃₁F₂N₃O₂	Melting Point	N/A
	MSDS	N/A	Flash Point	371.4±31.5 °C

Use of Zosuquidar

Zosuquidar (LY335979) is a potent negative modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM.IC50 value: 60 nM (Ki)Target: P-glycoproteinZosuquidar (LY335979) is a potent modulator of P-glycoprotein-mediated multidrug resistance with Ki of 60 nM. Zosuquidar binds with high affinity to P-glycoprotein and inhibits P-glycoprotein-mediated multidrug resistance (MDR). P-glycoprotein, encoded by the MDR-1 gene, is a member of the ATP-binding cassette superfamily of transmembrane transporters and prevents the intracellular accumulation of many natural product-derived cytotoxic agents. Zosuquidar is a compound of antineoplastic drug candidates currently under development.

Name	(2R)-1-{4-[(1aR,6r,10bS)-1,1-Difluoro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c]cyclohepten-6-yl]piperazin-1-yl}-3-(quinolin-5-yloxy)propan-2-ol
Synonym	More Synonyms

Description	Zosuquidar (LY335979) is a potent negative modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM.IC50 value: 60 nM (Ki)Target: P-glycoproteinZosuquidar (LY335979) is a potent modulator of P-glycoprotein-mediated multidrug resistance with Ki of 60 nM. Zosuquidar binds with high affinity to P-glycoprotein and inhibits P-glycoprotein-mediated multidrug resistance (MDR). P-glycoprotein, encoded by the MDR-1 gene, is a member of the ATP-binding cassette superfamily of transmembrane transporters and prevents the intracellular accumulation of many natural product-derived cytotoxic agents. Zosuquidar is a compound of antineoplastic drug candidates currently under development.
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> P-glycoprotein Research Areas >> Cancer
References	[1]. Dantzig AH, et al. Reversal of P-glycoprotein-mediated multidrug resistance by a potent cyclopropyldibenzosuberane modulator, LY335979. Cancer Res. 1996 Sep 15;56(18):4171-9. [2]. Marcelletti JF, Multani PS, Lancet JE et al. Leukemic blast and natural killer cell P-glycoprotein function and inhibition in a clinical trial of zosuquidar infusion in acute myeloid leukemia. Leuk Res. 2009 Jun;33(6):769-74. [3]. Ruff P, Vorobiof DA, Jordaan JP et al. A randomized, placebo-controlled, double-blind phase 2 study of docetaxel compared to docetaxel plus zosuquidar (LY335979) in women with metastatic or locally recurrent breast cancer who have received one prior chemotherapy regimen. Cancer Chemother Pharmacol. 2009 Sep;64(4):763-8. [4]. Cripe LD, Uno H, Paietta EM et al. Zosuquidar, a novel modulator of P-glycoprotein, does not improve the outcome of older patients with newly diagnosed acute myeloid leukemia: a randomized, placebo-controlled trial of the Eastern Cooperative Oncology Group 3999. Blood. 2010 Nov 18;116(20):4077-85. [5]. Abu Ajaj K, Graeser R, Kratz F. Zosuquidar and an albumin-binding prodrug of zosuquidar reverse multidrug resistance in breast cancer cells of doxorubicin and an albumin-binding prodrug of doxorubicin. Breast Cancer Res Treat. 2012 Jul;134(1):117-29.

Description

Related Catalog

Signaling Pathways >> Membrane Transporter/Ion Channel >> P-glycoprotein

Research Areas >> Cancer

References

[1]. Dantzig AH, et al. Reversal of P-glycoprotein-mediated multidrug resistance by a potent cyclopropyldibenzosuberane modulator, LY335979. Cancer Res. 1996 Sep 15;56(18):4171-9.

[2]. Marcelletti JF, Multani PS, Lancet JE et al. Leukemic blast and natural killer cell P-glycoprotein function and inhibition in a clinical trial of zosuquidar infusion in acute myeloid leukemia. Leuk Res. 2009 Jun;33(6):769-74.

[3]. Ruff P, Vorobiof DA, Jordaan JP et al. A randomized, placebo-controlled, double-blind phase 2 study of docetaxel compared to docetaxel plus zosuquidar (LY335979) in women with metastatic or locally recurrent breast cancer who have received one prior chemotherapy regimen. Cancer Chemother Pharmacol. 2009 Sep;64(4):763-8.

[4]. Cripe LD, Uno H, Paietta EM et al. Zosuquidar, a novel modulator of P-glycoprotein, does not improve the outcome of older patients with newly diagnosed acute myeloid leukemia: a randomized, placebo-controlled trial of the Eastern Cooperative Oncology Group 3999. Blood. 2010 Nov 18;116(20):4077-85.

[5]. Abu Ajaj K, Graeser R, Kratz F. Zosuquidar and an albumin-binding prodrug of zosuquidar reverse multidrug resistance in breast cancer cells of doxorubicin and an albumin-binding prodrug of doxorubicin. Breast Cancer Res Treat. 2012 Jul;134(1):117-29.

Density	1.4±0.1 g/cm3
Boiling Point	690.5±55.0 °C at 760 mmHg
Molecular Formula	C₃₂H₃₁F₂N₃O₂
Molecular Weight	527.604
Flash Point	371.4±31.5 °C
Exact Mass	527.238464
PSA	48.83000
LogP	4.30
Vapour Pressure	0.0±2.3 mmHg at 25°C
Index of Refraction	1.691
Storage condition	-20℃

Zosuquidar MSDS(Chinese)

(2R)-1-{4-[(1aR,10bS)-1,1-Difluoro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c][7]annulen-6-yl]piperazin-1-yl}-3-(quinolin-5-yloxy)propan-2-ol

Unii-ab5K82X98y

(2R)-1-{4-[(1aR,10bS)-1,1-Difluoro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c][7]annulen-6-yl]-1-piperazinyl}-3-(5-quinolinyloxy)-2-propanol

Zosuquidar

Zosuquidar [inn]

1-Piperazineethanol, 4-[(1aR,10bS)-1,1-difluoro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c]cyclohepten-6-yl]-α-[(5-quinolinyloxy)methyl]-, (αR)-

Shanghai Nianxing Industrial Co., Ltd
China
Product Name: Zosuquidar；LY335979
Price: Click To Check
Purity: 98.0%
Delivery: 10 Day
Contact: Yang
Email: sales@echemcloud.com

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Price: $125/10mM*1mLinDMSO

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Zosuquidar

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