| 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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- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
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.
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请回答明确,谢谢
装置是这样的:旋转蒸发仪上的冷凝管的水直接流到真空泵里以冷却真空泵然后再从真空泵里流出来.
现在的问题是,我第一天清洗过真空泵之后,第二天再用就发现真空泵里的水已经有股臭味了,有没有什么好的办法可以让它不臭?这样每天都处理的话,太浪费时间了.如果哪位有什么好主意的话,请告知,谢谢!
