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.
MedKoo Cat#: 202411
Name: R306465
CAS#: 604769-01-9
Chemical Formula: C19H19N5O4S
Exact Mass: 413.11
Molecular Weight: 413.45026
Elemental Analysis: C, 55.19; H, 4.63; N, 16.94; O, 15.48; S, 7.76
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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
The following data is based on the product molecular weight 413.45026 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 |
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.
