RG-2833 | RGFP-109 | CAS#1215493-56-3 | HDAC inhibitor

MedKoo Cat#: 406803 | Name: RG-2833

Description:

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

RG-2833, also known as RGFP-109, is a histone deacetylase inhibitor (HDACi). RG-2833 may be potentially useful for the neurodegenerative disease Friedreich ataxia (FRDA).

Chemical Structure

RG-2833

CAS#1215493-56-3

Theoretical Analysis

MedKoo Cat#: 406803

Name: RG-2833

CAS#: 1215493-56-3

Chemical Formula: C20H25N3O2

Exact Mass: 339.1947

Molecular Weight: 339.44

Elemental Analysis: C, 70.77; H, 7.42; N, 12.38; O, 9.43

Price and Availability

Size	Price	Availability
200mg	USD 550.00	2 Weeks
500mg	USD 950.00	2 Weeks
1g	USD 1,650.00	2 Weeks
2g	USD 2,650.00	2 Weeks

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Related CAS #

No Data

Synonym

RG-2833; RG 2833; RG2833; RGFP-109; RGFP 109; RGFP109.

IUPAC/Chemical Name

N-(6-(2-Aminophenylamino)-6-oxohexyl)-4-methylbenzamide

InChi Key

VOPDXHFYDJAYNS-UHFFFAOYSA-N

InChi Code

InChI=1S/C20H25N3O2/c1-15-10-12-16(13-11-15)20(25)22-14-6-2-3-9-19(24)23-18-8-5-4-7-17(18)21/h4-5,7-8,10-13H,2-3,6,9,14,21H2,1H3,(H,22,25)(H,23,24)

SMILES Code

O=C(NCCCCCC(NC1=CC=CC=C1N)=O)C2=CC=C(C)C=C2

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

>2 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

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

RG2833 is a brain-penetrant HDAC inhibitor with IC50s of 60 nM and 50 nM for HDAC1 and HDAC3, respectively. The Ki values for HDAC1 and HDAC3 are 32 and 5 nM, respectively.

In vitro activity:

To be determined

In vivo activity:

Pharmacological upregulation of SLFN11 by RG-2833 markedly increased sensitivity to cisplatin and SN-38 in SLFN11-negative medulloblastoma cells. High SLFN11 expression is one factor which renders favorable outcomes in WNT-activated and a subset of SHH-activated medulloblastoma possibly through enhancing response to cisplatin. Reference: Neuro Oncol. 2023 May 4;25(5):899-912. https://pubmed.ncbi.nlm.nih.gov/36273330/

	Solvent	mg/mL	mM
Solubility
	DMSO	100.0	299.11

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 339.44 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. Nakata S, Murai J, Okada M, Takahashi H, Findlay TH, Malebranche K, Parthasarathy A, Miyashita S, Gabdulkhaev R, Benkimoun I, Druillennec S, Chabi S, Hawkins E, Miyahara H, Tateishi K, Yamashita S, Yamada S, Saito T, On J, Watanabe J, Tsukamoto Y, Yoshimura J, Oishi M, Nakano T, Imamura M, Imai C, Yamamoto T, Takeshima H, Sasaki AT, Rodriguez FJ, Nobusawa S, Varlet P, Pouponnot C, Osuka S, Pommier Y, Kakita A, Fujii Y, Raabe EH, Eberhart CG, Natsumeda M. Epigenetic upregulation of Schlafen11 renders WNT- and SHH-activated medulloblastomas sensitive to cisplatin. Neuro Oncol. 2023 May 4;25(5):899-912. doi: 10.1093/neuonc/noac243. PMID: 36273330; PMCID: PMC10158119. 2. Soragni E, Miao W, Iudicello M, Jacoby D, De Mercanti S, Clerico M, Longo F, Piga A, Ku S, Campau E, Du J, Penalver P, Rai M, Madara JC, Nazor K, O'Connor M, Maximov A, Loring JF, Pandolfo M, Durelli L, Gottesfeld JM, Rusche JR. Epigenetic therapy for Friedreich ataxia. Ann Neurol. 2014 Oct;76(4):489-508. doi: 10.1002/ana.24260. Epub 2014 Sep 16. PMID: 25159818; PMCID: PMC4361037.

In vitro protocol:

To be determined

In vivo protocol:

1: Soragni E, Miao W, Iudicello M, Jacoby D, De Mercanti S, Clerico M, Longo F, Piga A, Ku S, Campau E, Du J, Penalver P, Rai M, Madara JC, Nazor K, O'Connor M, Maximov A, Loring JF, Pandolfo M, Durelli L, Gottesfeld JM, Rusche JR. Epigenetic therapy for Friedreich ataxia. Ann Neurol. 2014 Oct;76(4):489-508. doi: 10.1002/ana.24260. Epub 2014 Sep 16. PubMed PMID: 25159818; PubMed Central PMCID: PMC4361037.