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Tasisulam

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Tasisulam manufacturers

  • Tasisulam
  • Tasisulam pictures
  • $56.00
  • 2026-06-02
  • CAS:519055-62-0
  • Purity: 99.77%
  • Supply Ability: 10g
  • Tasisulam
  • Tasisulam pictures
  • $1.00
  • 2019-12-27
  • CAS:519055-62-0
  • Min. Order: 1KG
  • Purity: 97%-99.9%
  • Supply Ability: 100kg
Tasisulam Basic information
Product Name:Tasisulam
Synonyms:Benzamide, N-((5-bromo-2-thienyl)sulfonyl)-2,4-dichloro-;Ly573636;Ly-573636;TS81557;LY573636 (TasisulaM);Tasisulam(Ly-573636;N-(2,4-Dichlorobenzoyl)-5-bromothiophene-2-sulfonamide LY573636 Tasisulam;Tasisulam N-(2,4-Dichlorobenzoyl)-5-bromothiophene-2-sulfonamide
CAS:519055-62-0
MF:C11H6BrCl2NO3S2
MW:415.11
EINECS:
Product Categories:Inhibitors
Mol File:519055-62-0.mol
Tasisulam Structure
Tasisulam Chemical Properties
density 1.812
storage temp. Store at -20° C
solubility DMF: 20 mg/ml; DMSO: 20 mg/ml; Ethanol: 10 mg/ml; PBS (pH 7.2): 0.2 mg/ml
form A crystalline solid
pka3.45±0.10(Predicted)
color Light yellow to yellow
InChIInChI=1S/C11H6BrCl2NO3S2/c12-9-3-4-10(19-9)20(17,18)15-11(16)7-2-1-6(13)5-8(7)14/h1-5H,(H,15,16)
InChIKeyWWONFUQGBVOKOF-UHFFFAOYSA-N
SMILESC(NS(C1SC(Br)=CC=1)(=O)=O)(=O)C1=CC=C(Cl)C=C1Cl
Safety Information
WGK Germany WGK 3
Storage Class11 - Combustible Solids
MSDS Information
Tasisulam Usage And Synthesis
UsesThe sodium salt of Tasisulam has potential antineoplastic activity. Selectively toxic towards tumor cells, tasisulam appears to induce tumor cell apoptosis by a mitochondrial-targeted mechanism involving the loss of mitochondrial membrane potential and induction of reactive oxygen species (ROS).
Biological ActivityTasisulam (LY573636) is a SPLAM (SPLicing inhibitor sulfonAMide) th at bridges RNA binding motif protein 39 (RBM39; CAPERα, HCC1) and DCAF15 for interaction, thereby promoting (CUL4-DDB1-DDA1-DCAF15) E3 ubiquitin ligase complex-mediated RBM39 ubiquitination and subsequent proteasomal degradation. Tasisulam exerts selective toxicity in parental HCT116 cancer cultures (IC50 = 6.5 μM), but not those harboring non-CUL4-DCAF15-associating RBM39 G268V mutant even at a high concentration of 50 μM.
Synthesis
2,4-Dichlorobenzoic acid

50-84-0

2-Thiophenesulfonyl azide, 5-bromo-

1152981-12-8

Tasisulam

519055-62-0

General procedure for the synthesis of N-(2,4-dichlorobenzoyl)-5-bromothiophene-2-sulfonamide from 2,4-dichlorobenzoic acid and the compound (CAS:1152981-12-8): 0.5 mmol (0.0955 g) of 2,4-dichlorobenzoic acid, 0.75 mmol (0.2011 g) of 2-bromothiophene-sulfonamide azide, and 0.025 mmol (0.0086 g) octacarbonyldicobalt in a 25 mL reaction tube; subsequently, 4 mL of acetonitrile solvent was added via a microsyringe, and the reaction system was stirred at 80 °C for 4 hours. Upon completion of the reaction, the mixture was concentrated by rotary evaporation and purified by column chromatography (column conditions: 200-300 mesh silica gel, mobile phase ethyl acetate:petroleum ether=1:4) to give 0.1583 g of the target product as a white solid in 76% yield.

References[1] Chemistry--A European Journal, 2012, vol. 18, # 45, p. 14444 - 14453,10
[2] Chemistry - A European Journal, 2012, vol. 18, # 45, p. 14444 - 14453
[3] Journal of Organic Chemistry, 2018, vol. 83, # 16, p. 9364 - 9369
[4] Patent: CN108558822, 2018, A. Location in patent: Paragraph 0035; 0036; 0037; 0040; 0043
Tasisulam Preparation Products And Raw materials
Raw materials2,4-Dichlorobenzoic acid-->2-Thiophenesulfonyl azide, 5-bromo--->Cobalt carbonyl-->Acetonitrile-->tert-Butyl isocyanide
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