| SW203668stearoyl CoA desaturase 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.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
SW203668 Dilution Calculator
calculate
SW203668 Molarity Calculator
calculate
| Cas No. | 1673556-40-5 | SDF | Download SDF |
| Chemical Name | 4-(aminophenylmethyl)-N-(6-methoxy-2-benzothiazolyl)-benzamide | ||
| Canonical SMILES | COC1=CC=C2C(SC(NC(C3=CC=C(C(N)C4=CC=CC=C4)C=C3)=O)=N2)=C1 | ||
| Formula | C22H19N3O2S | M.Wt | 389.5 |
| Solubility | ≤20mg/ml in DMSO | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | 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: 0.022 μM for H2122 cells
SW203668 is a stearoyl CoA desaturase inhibitor.
The enzyme of stearoyl-CoA desaturase (SCD) is the rate-limiting enzyme in the synthesis of monounsaturated fatty acids such as palmitoleic acid and oleic acid, which are two most abundant monounsaturated fatty acids in human membranes, plasma lipids as well as adipose tissue. Though the endogenous synthesis of fatty acids in humans is not significant in most circumstances, it is increasingly becoming evident that SCD plays key structural and metabolic roles.
In vitro: By the screening, the optimized benzothiazole SW203668 was found to be selectively toxic to various cell lines (IC50 = 0.022-0.116 μM). Moreover, the ectopic expression of CYP4F11 in H1155, an SW203668-insensitive cell line, led to its sensitization to toxicity by SW203668 and therefore these results confirmed that CYP4F11 could also activate SW203668 [1].
In vivo: A PK analysis of SW203668 revealed that the plasma levels exceeded 0.3 μM for the first 6 h and a half-life of 8 h after an intraperitoneal injection at 25 mg/kg. Immunodeficient mice bear-ing 200 mm3 tumors derived either from H2122 cells (sensitive) or H1155 cells (insensitive) was intraperitoneally treated with 25 mg/kg of SW203668 twice a day for 10–15 d. Results showed that after administration of SW203668 a substantially reduced rate of growth in H2122-derived tumors was observed. While the H1155-derived tumors were unaffected, suggesting that the selectivity and cytotoxicity of SW203668 were maintained in vivo [1].
Clinical trial: So far, no clinical study has been conducted.
Reference:[1] Theodoropoulos PC et al. Discovery of tumor-specific irreversible inhibitors of stearoyl CoA desaturase. Nat Chem Biol. 2016 Apr;12(4):218-25.
