ChemicalBook > CAS DataBase List > RGFP 109

RGFP 109

Product Name
RGFP 109
CAS No.
1215493-56-3
Chemical Name
RGFP 109
Synonyms
RG2833;RG-2833;RG 2833;RGFP109;CS-2320;RGFP 109;RGFP-109;RG2833(RGFP109);RG2833, 10 mM in DMSO;RG2833 (RGFP109) ，S7292
CBNumber
CB02666680
Molecular Formula
C20H25N3O2
Formula Weight
339.43
MOL File
1215493-56-3.mol
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RGFP 109 Property

Boiling point:
620.1±50.0 °C(Predicted)
Density 
1.163±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
insoluble in H2O; ≥16.95 mg/mL in DMSO; ≥8.05 mg/mL in EtOH with gentle warming and ultrasonic
form 
Powder
pka
14.62±0.70(Predicted)
color 
White to off-white
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical
Product number
21568
Product name
RGFP109
Purity
≥98%
Packaging
5mg
Price
$62
Updated
2024/03/01
Cayman Chemical
Product number
21568
Product name
RGFP109
Purity
≥98%
Packaging
10mg
Price
$109
Updated
2024/03/01
Cayman Chemical
Product number
21568
Product name
RGFP109
Purity
≥98%
Packaging
25mg
Price
$225
Updated
2024/03/01
Cayman Chemical
Product number
21568
Product name
RGFP109
Purity
≥98%
Packaging
50mg
Price
$299
Updated
2024/03/01
Usbiological
Product number
464661
Product name
RGFP 109
Packaging
10mg
Price
$403
Updated
2021/12/16
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RGFP 109 Chemical Properties,Usage,Production

Uses

RGFP 109 is a histone deacetylase (HDAC) inhibitor that has shown to reverse FXN gene silencing in short-term studies of Friedreich ataxia (FRDA) patient cells.

Synthesis

95-54-5

78521-43-4

1215493-56-3

The general procedure for the synthesis of N-[6-(2-aminophenylamino)-6-oxohexyl]-4-methylbenzamide (R01) from o-phenylenediamine and 6-(4-methylbenzoylamino)hexanoic acid was as follows: under nitrogen protection, 6-(4-methylbenzoylamino)hexanoic acid (498 mg, 2 mmol), o-phenylenediamine (216 mg, 2 mmol), EDCI (383 mg, 2 mmol), HOBt (405 mg, 3 mmol) and triethylamine (404 mg, 4 mmol) were dissolved in dichloromethane (30 mL) and the reaction was stirred at room temperature. After completion of the reaction, the reaction mixture was washed with water and brine, dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography to afford the target compound N-[6-(2-aminophenylamino)-6-oxohexyl]-4-methylbenzamide (227 mg, 33.9% yield) as a white solid. The product was confirmed to be >95% pure by 1H NMR (DMSO-d6) and LC-MS characterization.1H NMR (DMSO-d6) δ: 9.06 (s, 1H), 8.35 (s, 1H), 7.73 (d, J = 8.0 Hz, 2H), 7.24 (d, J = 8.0 Hz, 2H), 7.14 (t, J = 7.5 Hz, 1H), 6.86-6.89 (m, 1H), 6.70 (d, J = 7.5 Hz, 1H), 6.50 (t, J = 7.5 Hz, 1H), 4.80 (s, 2H), 3.22-3.26 (m, 2H), 2.30-2.35 (m, 5H), 1.53-1.65 (m, 4H), 1.36-1.38 (m, 2H). LC-MS (ESI): m/z 340 [M+H]+.

in vivo

RG2833 (150 mg/kg) is able to correct frataxin deficiency in the brain and heart of KIKI mice 24 hours after a single injection, but not when lower doses are used. When followed in time, the frataxin mRNA increase induced by RG2833 in the KIKI mouse can be first detected at 12 hours and reach a maximum at 24 hours in both brain and heart[1]. RG2833 (100 mg/kg, s.c.) is well tolerated in chronic dosing of mice without toxicity. RG2833 improves motor coordination of YG8R FRDA mice. RG2833 increases frataxin protein expression in the brain of YG8R FRDA mice[2]. RGFP109 (30 mg/kg, p.o. once daily for 6 days) has no acute effects on dyskinesia after single or 6 days once-daily treatment. One week following cessation of RGFP109, dyskinesia and duration of ON-time with disabling dyskinesia are reduced by 37% and 50%, respectively[3].

target

HDAC1

IC 50

HDAC3: 50 nM (IC50); HDAC1: 60 nM (IC50); HDAC3: 5 nM (Ki); HDAC1: 32 nM (Ki)

References

[1] Patent: US2012/94971, 2012, A1. Location in patent: Page/Page column 40

RGFP 109 Preparation Products And Raw materials

Raw materials

Preparation Products

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RGFP 109 Suppliers

China 103 India 2 United States 14 Global 119
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Cckinase, Inc.
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1215493-56-3, RGFP 109Related Search:

TYRPHOSTIN RG 13022 CTEP Derivative N-PHTHALYL-1-TRYPTOPHAN N,N-DIETHYLBENZAMIDE TRICHOSTATIN A Tacedinaline JNJ-26481585 Vorinostat (1S,4Z,7S,10S,11E,20R)-4-ethylidene-7,20-dipropan-2-yl-9-oxa-15,16-dit hia-3,6,18,21-tetrazabicyclo[8.7.6]tricos-11-ene-2,5,8,19,22-pentone RGFP966

  • RGFP 109 N-[6-(2-Aminophenylamino)-6-oxohexyl]-4-methylbenzamide
  • RG 2833
  • RG2833
  • RG-2833
  • RGFP 109
  • RGFP109
  • RGFP-109
  • RG2833(RGFP109)
  • N-[6-(2-Aminophenylamino)-6-oxohexyl]-4-methylbenzamide
  • N-[6-(2-aminoanilino)-6-oxohexyl]-4-methylbenzamide
  • RG2833; RGFP109; RG-2833; RGFP 109
  • CS-2320
  • Benzamide, N-[6-[(2-aminophenyl)amino]-6-oxohexyl]-4-methyl-
  • RGFP109 RG-2833 RGFP-109 RG2833
  • RG2833, 10 mM in DMSO
  • RG2833 (RGFP109) ，S7292
  • 1215493-56-3
  • Inhibitors