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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
Molecular Weight:
618.57
MDL Number:
MFCD26523136
MOL File:
1561178-17-3.mol
MSDS File:
SDS
Last updated:2023-06-30 15:45:59

SGC0946 Properties

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

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS06
Signal word  Danger
Hazard statements  H301
Precautionary statements  P301+P310
Hazard Codes  T
Risk Statements  25
Safety Statements  45
RIDADR  UN 2811 6.1 / PGIII
WGK Germany  3
HS Code  2934999090
NFPA 704
0
2 0

SGC0946 price More Price(30)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich SML1107 SGC0946 ≥98% (HPLC) 1561178-17-3 5mg $154 2024-03-01 Buy
Sigma-Aldrich SML1107 SGC0946 ≥98% (HPLC) 1561178-17-3 25mg $462 2024-03-01 Buy
Cayman Chemical 13967 SGC0946 ≥98% 1561178-17-3 5mg $96 2024-03-01 Buy
Cayman Chemical 13967 SGC0946 ≥98% 1561178-17-3 10mg $182 2024-03-01 Buy
Cayman Chemical 13967 SGC0946 1561178-17-3 25mg $380 2024-03-01 Buy
Product number Packaging Price Buy
SML1107 5mg $154 Buy
SML1107 25mg $462 Buy
13967 5mg $96 Buy
13967 10mg $182 Buy
13967 25mg $380 Buy

SGC0946 Chemical Properties,Uses,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

Global( 114)Suppliers
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ATK CHEMICAL COMPANY LIMITED
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InvivoChem
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+undefined18051384581 sales@chemhifuture.com China 3136 58
TargetMol Chemicals Inc.
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SGC0946 Spectrum

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 CS-1475 CS-1937 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