NSC23925 | CAS#858474-14-3 | Pgp1 inhibitor

MedKoo Cat#: 558408 | Name: NSC23925

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

NSC23925 is a plasma membrane glycoprotein 1 (Pgp1) inhibitor to reverse multidrug resistance (MDR1). Findings suggest that NSC23925 can prevent the emergence of MDR in ovarian cancer both in vitro and in vivo. The clinical use of NSC2395 at the onset of chemotherapy may prevent the development of MDR and improve the clinical outcome of patients with ovarian cancer.

Chemical Structure

NSC23925

CAS#858474-14-3

Theoretical Analysis

MedKoo Cat#: 558408

Name: NSC23925

CAS#: 858474-14-3

Chemical Formula: C22H26Cl2N2O2

Exact Mass: 420.1371

Molecular Weight: 421.36

Elemental Analysis: C, 62.71; H, 6.22; Cl, 16.83; N, 6.65; O, 7.59

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 260.00
10mg	USD 420.00
25mg	USD 730.00

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Related CAS #

No Data

Synonym

NSC23925; NSC-23925; NSC 23925;

IUPAC/Chemical Name

2-(p-Methoxyphenyl)-α-2-piperidyl-4-quinolinemethanol Dihydrochloride

InChi Key

WGWOQHWZXLGPNG-UHFFFAOYSA-N

InChi Code

InChI=1S/C22H24N2O2.2ClH/c1-26-16-11-9-15(10-12-16)21-14-18(17-6-2-3-7-19(17)24-21)22(25)20-8-4-5-13-23-20;;/h2-3,6-7,9-12,14,20,22-23,25H,4-5,8,13H2,1H3;2*1H

SMILES Code

OC(C1NCCCC1)C2=CC(C3=CC=C(OC)C=C3)=NC4=CC=CC=C24.[H]Cl.[H]Cl

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.03.00

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

NSC23925 is a novel, selective and effective P-glycoprotein (Pgp) inhibitor.

In vitro activity:

This study found that at a concentration of >10 microM NSC23925 moderately inhibits the proliferation of both sensitive and resistant cell lines with almost equal activity, but its inhibitory effect was not altered by co-incubation with the Pgp1 inhibitor, verapamil, suggesting that NSC23925 itself is not a substrate of Pgp1. Additionally, NSC23925 increases the intracellular accumulation of Pgp1 substrates: calcein AM, Rhodamine-123, paclitaxel, mitoxantrone, and doxorubicin. Reference: PLoS One. 2009 Oct 12;4(10):e7415. https://pubmed.ncbi.nlm.nih.gov/19823672/

In vivo activity:

The majority of mice continuously treated with paclitaxel alone eventually developed paclitaxel resistance with overexpression of Pgp and antiapoptotic proteins, whereas mice remained sensitivity to paclitaxel and displayed lower expression levels of Pgp and antiapoptotic proteins after administered continuously with combination of paclitaxel-NSC23925. Paclitaxel-NSC23925-treated mice experienced significantly longer overall survival time than paclitaxel-treated mice. Furthermore, the combination of paclitaxel and NSC23925 therapy did not induce obvious toxicity as measured by mice body weight changes, blood cell counts and histology of internal organs. Reference: Int J Cancer. 2015 Oct 15;137(8):2029-39. https://pubmed.ncbi.nlm.nih.gov/25904021/

	Solvent	mg/mL	mM
Solubility
	Water	4.0	9.49

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 421.36 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Yang X, Feng Y, Gao Y, Shen J, Choy E, Cote G, Harmon D, Zhang Z, Mankin H, Hornicek FJ, Duan Z. NSC23925 prevents the emergence of multidrug resistance in ovarian cancer in vitro and in vivo. Gynecol Oncol. 2015 Apr;137(1):134-42. doi: 10.1016/j.ygyno.2015.02.002. Epub 2015 Feb 10. PMID: 25677062. 2. Duan Z, Choy E, Hornicek FJ. NSC23925, identified in a high-throughput cell-based screen, reverses multidrug resistance. PLoS One. 2009 Oct 12;4(10):e7415. doi: 10.1371/journal.pone.0007415. PMID: 19823672; PMCID: PMC2757897. 3. Yang X, Shen J, Gao Y, Feng Y, Guan Y, Zhang Z, Mankin H, Hornicek FJ, Duan Z. Nsc23925 prevents the development of paclitaxel resistance by inhibiting the introduction of P-glycoprotein and enhancing apoptosis. Int J Cancer. 2015 Oct 15;137(8):2029-39. doi: 10.1002/ijc.29574. Epub 2015 May 5. PMID: 25904021; PMCID: PMC4529776.

In vitro protocol:

In vivo protocol:

1. Yang X, Shen J, Gao Y, Feng Y, Guan Y, Zhang Z, Mankin H, Hornicek FJ, Duan Z. Nsc23925 prevents the development of paclitaxel resistance by inhibiting the introduction of P-glycoprotein and enhancing apoptosis. Int J Cancer. 2015 Oct 15;137(8):2029-39. doi: 10.1002/ijc.29574. Epub 2015 May 5. PMID: 25904021; PMCID: PMC4529776.

1: Yang X, Yang P, Shen J, Osaka E, Choy E, Cote G, Harmon D, Zhang Z, Mankin H, Hornicek FJ, Duan Z. Prevention of multidrug resistance (MDR) in osteosarcoma by NSC23925. Br J Cancer. 2014 Jun 10;110(12):2896-904. doi: 10.1038/bjc.2014.254. Epub 2014 May 22. PubMed PMID: 24853187; PubMed Central PMCID: PMC4056062. 2: Yang X, Feng Y, Gao Y, Shen J, Choy E, Cote G, Harmon D, Zhang Z, Mankin H, Hornicek FJ, Duan Z. NSC23925 prevents the emergence of multidrug resistance in ovarian cancer in vitro and in vivo. Gynecol Oncol. 2015 Apr;137(1):134-42. doi: 10.1016/j.ygyno.2015.02.002. Epub 2015 Feb 10. PubMed PMID: 25677062. 3: Yang X, Shen J, Gao Y, Feng Y, Guan Y, Zhang Z, Mankin H, Hornicek FJ, Duan Z. Nsc23925 prevents the development of paclitaxel resistance by inhibiting the introduction of P-glycoprotein and enhancing apoptosis. Int J Cancer. 2015 Oct 15;137(8):2029-39. doi: 10.1002/ijc.29574. Epub 2015 May 5. PubMed PMID: 25904021; PubMed Central PMCID: PMC4529776. 4: Duan Z, Choy E, Hornicek FJ. NSC23925, identified in a high-throughput cell-based screen, reverses multidrug resistance. PLoS One. 2009 Oct 12;4(10):e7415. doi: 10.1371/journal.pone.0007415. PubMed PMID: 19823672; PubMed Central PMCID: PMC2757897. 5: Duan Z, Li X, Huang H, Yuan W, Zheng SL, Liu X, Zhang Z, Choy E, Harmon D, Mankin H, Hornicek F. Synthesis and evaluation of (2-(4-methoxyphenyl)-4-quinolinyl)(2-piperidinyl)methanol (NSC23925) isomers to reverse multidrug resistance in cancer. J Med Chem. 2012 Apr 12;55(7):3113-21. doi: 10.1021/jm300117u. Epub 2012 Mar 22. PubMed PMID: 22400811. 6: Gao Y, Shen JK, Choy E, Zhang Z, Mankin HJ, Hornicek FJ, Duan Z. Pharmacokinetics and tolerability of NSC23925b, a novel P-glycoprotein inhibitor: preclinical study in mice and rats. Sci Rep. 2016 May 9;6:25659. doi: 10.1038/srep25659. PubMed PMID: 27157103; PubMed Central PMCID: PMC4860631.