| Identification | Back Directory | [Name]
N,N'-[Sulfonylbis(1,4-phenylene)]bis(chloroacetamide) | [CAS]
17328-16-4 | [Synonyms]
TC-E 5003
N'-(Sulfonyldi-4
TC-E 5003 (NSC-30176)
1-phenylene)bis(2-chloroacetamide)
4',4'''-Sulfonylbis(α-chloroacetanilide)
Bis[4-(chloroacetylamino)phenyl] sulfone
N,N'-[Sulfonylbis(1,4-phenylene)]bis(chloroacetamide)
N,N'-(Sulfonyldi-4,1-phenylene)bis(2-chloroacetamide)
N,N'-[Sulfonylbis(4,1-phenylene)]bis(2-chloroacetamide) | [Molecular Formula]
C16H14Cl2N2O4S | [MDL Number]
MFCD00028183 | [MOL File]
17328-16-4.mol | [Molecular Weight]
401.26 |
| Chemical Properties | Back Directory | [Melting point ]
191-192 °C | [Boiling point ]
704.2±60.0 °C(Predicted) | [density ]
1.504±0.06 g/cm3(Predicted) | [storage temp. ]
-20°C (des.) | [solubility ]
Soluble in DMSO (up to 50 mg/ml). | [form ]
solid | [pka]
11.56±0.70(Predicted) | [color ]
Brown | [Stability:]
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month. |
| Hazard Information | Back Directory | [Description]
TC-E 5003 is an inhibitor of protein arginine methyltransferase 1 (PRMT1; IC50 = 1.5 μM for human PRMT1 in a methylation assay). It is selective for PRMT1 over PRMT4/CARM1 and SET7/9 methyltransferases, with less than 5% inhibition at a concentration of 50 μM for SET7/9. TC-E 5003 inhibits growth of MCF-7a breast cancer and LNCaP prostate cancer cells (GI50s = 1.97 and 4.49 μM, respectively) and decreases androgen-dependent gene transcription in vitro. TC-E 5003 (80 mg/kg) also has antimalarial properties and eradicates P. berghei in mice. | [Uses]
NSC 30176 is a inhibitor of human PRMT1, it is selective for PRMT1 over the arginine methyltransferase CARM1 and the lysine methyltransferase Set7/9. | [in vivo]
TC-E 5003 (0.5-2.0 mg, s.c., a single dose for 28 days) has an excellent tumor-suppressing effect in A549 tumor xenograft ICR mouse models [3].
| Animal Model: | A549 tumor xenograft ICR mouse model[3] | | Dosage: | 0.5-2.0 mg | | Administration: | s.c., a single dose for 28 days | | Result: | Achieved better antitumor effect in combination with INEI system in A549 tumor xenograft ICR mouse model. |
| [IC 50]
PRMT1 | [storage]
Store at -20°C | [References]
1) Bissinger?et al. (2011),?Acyl derivatives of p-aminosulfonamides and dapsone as new inhibitors of the arginine methytransferase hPRMT1; Bioorg. Med. Chem.,?19?3717 |
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