| CB30865Nampt inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
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- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
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Chemical structure
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| Cas No. | 206275-15-2 | SDF | Download SDF |
| Synonyms | ZM242421;CB-30865;CB 30865;ZM-242421;ZM 242421 | ||
| Chemical Name | 4-[(7-bromo-2-methyl-4-oxo-1H-quinazolin-6-yl)methyl-prop-2-ynylamino]-N-(pyridin-3-ylmethyl)benzamide | ||
| Canonical SMILES | CC1=NC(=O)C2=CC(=C(C=C2N1)Br)CN(CC#C)C3=CC=C(C=C3)C(=O)NCC4=CN=CC=C4 | ||
| Formula | C26H22BrN5O2 | M.Wt | 516.39 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
IC50: 2.8 nM for W1L2; 156 nM for isolated mammalian TS
CB30865 is a highly potent cytotoxic agent. The compound inhibits isolated mammalian thymidylate synthase (TS), but this inhibition is insufficient to account for its cellular toxicity. Thymidylate synthase (TS) is a critical enzyme in the de novo synthesis of thymidylate (dTTP) and has long been recognized as a target for chemotherapeutic intervention.
In vitro: CB30865 was the most potent growth inhibitory agent (IC50 values in the range 1–100 nM for several mouse and human cell types). Against W1L2 cells, the analogues of CB300179 and CB300189 demonstrated reduced potency in the presence of exogenous thymidine (dThd), and against a W1L2:C1 TS overproducing cell line. In contrast, CB30865 retained activity in these systems. No cell cycle redistribution was observed following exposure (4–48 h) to an equitoxic concentration of CB30865[1].
In vivo: The in vivo evaluation of CB30865 was hampered because of its low aqueous solubility (<1 μm="" at="" ph="" 6).="" this="" low="" aqueous="" solubility="" of="" cb30865="" initiated="" a="" search="" for="" more="" water-soluble="" analogues="" to="" allow="" the="" in="" vivo="" evaluation="" of="" this="" class="" of="" compounds.="" it="" was="" envisaged="" that="" aqueous="" solubility="" could="" be="" increased="" by="" the="" introduction="" of="" amino="" functionalities="" (e.g.,="" n-methylpiperazine)="" at="" the="" 2-position="" of="" the="" quinazolin-4-one="" ring="" [2].="">
Clinical trial: No clinical data are available
References:[1] Bavetsias V, Skelton LA, Yafai F, Mitchell F, Wilson SC, Allan B, Jackman AL. The design and synthesis of water-soluble analogues of CB30865, a quinazolin-4-one-based antitumor agent. J Med Chem. 2002;45(17):3692-702.[2] Skelton LA, Ormerod MG, Titley J, Kimbell R, Brunton LA, Jackman AL. A novel class of lipophilic quinazoline-based folic acid analogues: cytotoxic agents with a folate-independent locus. Br J Cancer. 1999;79(11-12):1692-701.
