SGC0946

ChemicalBook > CAS DataBase List > SGC0946

Product Name: SGC0946
CAS No.: 1561178-17-3
Chemical Name: SGC0946
Synonyms: sg946;CS-1937;CS-1475;SGC0946;SGC0946 USP/EP/BP;1-(3-((((2R,3S,4R,5R)-5-(4-Amino-5-bromo-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydroxytetrahy;5-Bromo-7-[5-deoxy-5-[[3-[[[[4-(1,1-dimethylethyl)phenyl]amino]carbonyl]amino]propyl](1-methylethyl)amino]-beta-D-7H-Pyrrolo[2,3-;5-Bromo-7-[5-deoxy-5-[[3-[[[[4-(1,1-dimethylEthyl)phenyl]amino]carbonyl]amino]propyl](1-methylEthyl)amino]-β-D-ribofuranosyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine;7H-Pyrrolo[2,3-d]pyrimidin-4-amine, 5-bromo-7-[5-deoxy-5-[[3-[[[[4-(1,1-dimethylethyl)phenyl]amino]carbonyl]amino]propyl](1-methylethyl)amino]-β-D-ribofuranosyl]-;5-Bromo-7-[5-deoxy-5-[[3-[[[[4-(1,1-dimethylethyl)phenyl]amino]carbonyl]amino]propyl](1-methylethyl)amino]-beta-D-ribofuranosyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine
CBNumber: CB32645673
Molecular Formula: C28H40BrN7O4
Formula Weight: 618.57
MOL File: 1561178-17-3.mol

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SGC0946 Property

Melting point:: 125-126o C
Boiling point:: 771.5±60.0 °C(Predicted)
Density: 1.48±0.1 g/cm3(Predicted)
storage temp.: -20°C
solubility: DMSO: soluble20mg/mL, clear
pka: 12.39±0.70(Predicted)
form: powder
color: white to beige

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Safety

Hazard Codes: T
Risk Statements: 25
Safety Statements: 45
RIDADR: UN 2811 6.1 / PGIII
WGK Germany: 3
HS Code: 2934999090

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word: Danger
Hazard statements: H301Toxic if swalloed
Precautionary statements: P301+P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML1107
Product name: SGC0946
Purity: ≥98% (HPLC)
Packaging: 5mg
Price: $154
Updated: 2024/03/01

Sigma-Aldrich

Product number: SML1107
Product name: SGC0946
Purity: ≥98% (HPLC)
Packaging: 25mg
Price: $462
Updated: 2024/03/01

Cayman Chemical

Product number: 13967
Product name: SGC0946
Purity: ≥98%
Packaging: 5mg
Price: $96
Updated: 2024/03/01

Cayman Chemical

Product number: 13967
Product name: SGC0946
Purity: ≥98%
Packaging: 10mg
Price: $182
Updated: 2024/03/01

Cayman Chemical

Product number: 13967
Product name: SGC0946
Packaging: 25mg
Price: $380
Updated: 2024/03/01

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SGC0946 Chemical Properties,Usage,Production

Uses

SGC0946 is a potent DOT1L methyltransferase inhbiitor used in the treatment of leukemia seen effectively in vitro.

Biological Activity

sgc 0946 is a potent small-molecule inhibitor of protein methyltransferase (pmt) dot1l, a unique protein lysine methyltransferase (pkmt) catalyzing the methylation of histone h3 on lysine 79 (h3k79), with the half maximal inhibition concentration ic50 value of 0.3 nm [1].as a brominated analogue of epz004777, sgc 0946 exhibits substantially increased cellular inhibitory potency than its predecessor, where sgc 0946 reduces the methylation of h3k79 in both mcf10a (ic50: 8.8 nm) and a431 (ic50: 2.65 nm) cells compared with epz004777 (ic50: 84 nm and 264 nm respectively). this greatly increased cellular inhibitory potency of sgc 0946 can be attributed to lower off-rate and to improved cell permeability [1].

Biochem/physiol Actions

SGC0946 is a potent and selective inhibitor of Histone H3-lysine79 (H3K79) methyltransferase DOT1L with an IC50 of 0.3 nM in a radioactive enzyme assay, and over 100-fold selectivity for DOT1L over other histone methyltransferases. In cell studies, SGC0946 reduces H3K79 dimethylation with an IC50 of 2.6 nM in A431 cells and 8.8 nM in MCF10A cells. SGC0946 was found to selectively kills cells transformed with the MLL-AF9 fusion oncogene in an in vitro model of leukemia. For full characterization details, please visit the SGC0946 probe summary on the Structural Genomics Consortium (SGC) website.SGC0649 is the negative control for the active probe, SGC0946. To request a sample of the negative control from the SGC, click here.To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc

target

DOT1L

storage

Store at -20°C

SGC0946 Preparation Products And Raw materials

Raw materials

Preparation Products

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1561178-17-3, SGC0946Related Search:

1-Piperazinecarboxylic acid, 4-[3-amino-6-(2-hydroxyphenyl)-4-pyridazinyl]-, 1,1-dimethylethyl ester SGC-GAK-1 SGC2085 SGC707 SGC2085 EPZ004777 Tazemetostat (EPZ-6438) GSK J4 HCl GSK 343 (2R,3R,4S,5R)-2-(6-aMino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]iMidazol-2-yl)ethyl)cyclobutyl)(isopropyl)aMino)Methyl)tetrahydrofuran-3,4-diol 1-Cyclopentyl-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-6-(4-(MorpholinoMethyl)phenyl)-1H-indazole-4-carboxaMide

CS-1475

CS-1937

5-Bromo-7-[5-deoxy-5-[[3-[[[[4-(1,1-dimethylethyl)phenyl]amino]carbonyl]amino]propyl](1-methylethyl)amino]-beta-D-ribofuranosyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine

1-(3-((((2R,3S,4R,5R)-5-(4-Amino-5-bromo-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydroxytetrahy

SGC0946

1-(3-((((2R,3S,4R,5R)-5-(4-Amino-5-bromo-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl)(isopropyl)amino)propyl)-3-(4-(tert-butyl)phenyl)urea

5-Bromo-7-[5-deoxy-5-[[3-[[[[4-(1,1-dimethylethyl)phenyl]amino]carbonyl]amino]propyl](1-methylethyl)amino]-beta-D-7H-Pyrrolo[2,3-

1-[3-[[[(2R,3S,4R,5R)-5-(4-Amino-5--bromo-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydro-xytetrahydrofuran-2-yl]methyl](isopropyl)amino]pro-pyl]-3-[4-(2,2-dimethylethyl)phenyl]urea

7H-Pyrrolo[2,3-d]pyrimidin-4-amine, 5-bromo-7-[5-deoxy-5-[[3-[[[[4-(1,1-dimethylethyl)phenyl]amino]carbonyl]amino]propyl](1-methylethyl)amino]-β-D-ribofuranosyl]-

SGC0946 USP/EP/BP

sg946

5-Bromo-7-[5-deoxy-5-[[3-[[[[4-(1,1-dimethylEthyl)phenyl]amino]carbonyl]amino]propyl](1-methylEthyl)amino]-β-D-ribofuranosyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine

1561178-17-3

561178-17-3

C28H40BrN7O4

Inhibitors