R306465

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

MedKoo CAT#: 202411

CAS#: 604769-01-9

Description: R306465, also known as JNJ-16241199, is a novel hydroxamate-based histone deacetylase (HDAC) inhibitor with broad-spectrum antitumour activity against solid and haematological malignancies in preclinical models. R306465 was found to be a potent inhibitor of HDAC1 and -8 (class I) in vitro. R306465 potently inhibited cell proliferation of all main solid tumour indications, including ovarian, lung, colon, breast and prostate cancer cell lines, with IC50 values ranging from 30 to 300 nM. The high activity of R306465 in cell-based assays and in vivo after oral administration makes R306465 a promising novel antitumoral agent with potential applicability in a broad spectrum of human malignancies.

Chemical Structure

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R306465
CAS# 604769-01-9
Instruction

Theoretical Analysis

MedKoo Cat#: 202411
Name: R306465
CAS#: 604769-01-9
Chemical Formula: C19H19N5O4S
Exact Mass: 413.11
Molecular Weight: 413.450
Elemental Analysis: C, 55.19; H, 4.63; N, 16.94; O, 15.48; S, 7.76

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Synonym: R 306465; R306465; R-306465; JNJ16241199; JNJ-16241199; JNJ 16241199.

IUPAC/Chemical Name: N-hydroxy-2-(4-(naphthalen-2-ylsulfonyl)piperazin-1-yl)pyrimidine-5-carboxamide

InChi Key: MUTBJZVSRNUIHA-UHFFFAOYSA-N

InChi Code: InChI=1S/C19H19N5O4S/c25-18(22-26)16-12-20-19(21-13-16)23-7-9-24(10-8-23)29(27,28)17-6-5-14-3-1-2-4-15(14)11-17/h1-6,11-13,26H,7-10H2,(H,22,25)

SMILES Code: O=C(C1=CN=C(N2CCN(S(=O)(C3=CC=C4C=CC=CC4=C3)=O)CC2)N=C1)NO

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:        

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 413.45 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.

Recalculate based on batch purity %
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:
In vitro protocol:
In vivo protocol:

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 1. Angibaud, Patrick; Van Emelen, Kristof; Decrane, Laurence; van Brandt, Sven; ten Holte, Peter; Pilatte, Isabelle; Roux, Bruno; Poncelet, Virginie; Speybrouck, David; Queguiner, Laurence; Gaurrand, Sandrine; Marien, Ann; Floren, Wim; Janssen, Lut; Verdonck, Marc; van Dun, Jacky; van Gompel, Jacky; Gilissen, Ron; Mackie, Claire; Du Jardin, Marc; Peeters, Jozef; Noppe, Marc; Van Hijfte, Luc; Freyne, Eddy; Page, Martin; Janicot, Michel; Arts, Janine. Identification of a series of substituted 2-piperazinyl-5-pyrimidylhydroxamic acids as potent histone deacetylase inhibitors. Bioorganic & Medicinal Chemistry Letters (2010), 20(1), 294-298.

2. Brodie, Angela; Njar, Vincent C. O.; Sabnis, Gauri; Gediya, Lalji. HDAC inhibitors and hormone targeted drugs for the treatment of cancer. PCT Int. Appl. (2008), 96pp. CODEN: PIXXD2 WO 2008154402 A2 20081218

3. Arts, J.; Angibaud, P.; Marien, A.; Floren, W.; Janssens, B.; King, P.; van Dun, J.; Janssen, L.; Geerts, T.; Tuman, R. W.; Johnson, D. L.; Andries, L.; Jung, M.; Janicot, M.; van Emelen, K. R306465 is a novel potent inhibitor of class I histone deacetylases with broad-spectrum antitumoral activity against solid and hematological malignancies. British Journal of Cancer (2007), 97(10), 1344-1353.

4. Van Brandt, Sven Franciscus Anna; Van Emelen, Kristof; Angibaud, Patrick Rene; Marconnet-Decrane, Laurence Francoise Bernadette; Arts, Janine. Preparation of substituted propenyl piperazine derivatives as novel inhibitors of histone deacetylase. PCT Int. Appl. (2006), 67 pp. CODEN: PIXXD2 WO 2006010749 A2 20060202

5. Arts J; Angibaud P; Marien A; Floren W; Janssens B; King P; van Dun J; Janssen L; Geerts T; Tuman R W; Johnson D L; Andries L; Jung M; Janicot M; van Emelen K R306465 is a novel potent inhibitor of class I histone deacetylases with broad-spectrum antitumoral activity against solid and haematological malignancies. British journal of cancer (2007), 97(10), 1344-53.