SGC 0946

Modify Date: 2024-01-02 18:47:27

SGC 0946 Structure
SGC 0946 structure
Common Name SGC 0946
CAS Number 1561178-17-3 Molecular Weight 618.566
Density 1.5±0.1 g/cm3 Boiling Point 771.5±60.0 °C at 760 mmHg
Molecular Formula C28H40BrN7O4 Melting Point N/A
MSDS Chinese USA Flash Point 420.4±32.9 °C
Symbol GHS06
GHS06
Signal Word Danger

 Use of SGC 0946


SGC0946 is a highly potent and selective DOT1L methyltransferase inhibitor with IC50 of 0.3 nM; selectively kill mixed lineage leukaemia cells.IC50 value: 0.3 nM(DOT1L) [1]Target: selective DOT1L inhibitorSGC 0946 is over 100-fold selective for other histone methyltransferases/HMTs. SGC 0946 potently reduces H3K79 dimethylation with IC50 of 2.6 nM in A431 cells, and 8.8 nM in MCF10A cells, which potently and selectively kills cells containing an MLL translocation. SGC 0946 is much more potent than its close analog EPZ004777, and serves as an excellent chemical probe for investigating DOT1L and further development of DOT1L inhibitors for cancer therapy.

 Names

Name 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
Synonym More Synonyms

 SGC 0946 Biological Activity

Description SGC0946 is a highly potent and selective DOT1L methyltransferase inhibitor with IC50 of 0.3 nM; selectively kill mixed lineage leukaemia cells.IC50 value: 0.3 nM(DOT1L) [1]Target: selective DOT1L inhibitorSGC 0946 is over 100-fold selective for other histone methyltransferases/HMTs. SGC 0946 potently reduces H3K79 dimethylation with IC50 of 2.6 nM in A431 cells, and 8.8 nM in MCF10A cells, which potently and selectively kills cells containing an MLL translocation. SGC 0946 is much more potent than its close analog EPZ004777, and serves as an excellent chemical probe for investigating DOT1L and further development of DOT1L inhibitors for cancer therapy.
Related Catalog
References

[1]. Yu W, et al. Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors. Nat Commun. 2012;3:1288. doi: 10.1038/ncomms2304.

 Chemical & Physical Properties

Density 1.5±0.1 g/cm3
Boiling Point 771.5±60.0 °C at 760 mmHg
Molecular Formula C28H40BrN7O4
Molecular Weight 618.566
Flash Point 420.4±32.9 °C
Exact Mass 617.232483
LogP 4.72
Appearance of Characters white to beige
Vapour Pressure 0.0±2.8 mmHg at 25°C
Index of Refraction 1.662
Storage condition ?20°C
Water Solubility DMSO: soluble20mg/mL, clear

 Safety Information

Symbol GHS06
GHS06
Signal Word Danger
Hazard Statements H301
Precautionary Statements P301 + P310
Hazard Codes T
Risk Phrases 25
Safety Phrases 45
RIDADR UN 2811 6.1 / PGIII

 Synonyms

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-{isopropyl[3-({[4-(2-methyl-2-propanyl)phenyl]carbamoyl}amino)propyl]amino}-β-D-ribofuranosyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
sgc 0946
SGC0946
Top Suppliers:I want be here
  • DC Chemicals Limited
  • China
  • Product Name: SGC-0946
  • Price: $650.0/100mg $1300.0/250mg $2800.0/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao

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Price: $98/10mM*1mLinDMSO

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