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SGC 0946
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SGC 0946图片
CAS NO:1561178-17-3
规格:≥98%
包装与价格:
包装价格(元)
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)618.57
FormulaC28H40BrN7O4
CAS No.1561178-17-3
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 100 mg/mL (161.6 mM)
Water:<1 mg/mL
Ethanol: 100 mg/mL (161.6 mM)
Other infoChemical Name: 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-isobutylphenyl)urea
InChi Key: UZLAJVZJBSZSJL-VBHAUSMQSA-N
InChi Code: InChI=1S/C28H40BrN7O4/c1-16(2)12-18-6-8-19(9-7-18)34-28(39)31-10-5-11-35(17(3)4)14-21-23(37)24(38)27(40-21)36-13-20(29)22-25(30)32-15-33-26(22)36/h6-9,13,15-17,21,23-24,27,37-38H,5,10-12,14H2,1-4H3,(H2,30,32,33)(H2,31,34,39)/t21-,23-,24-,27-/m1/s1
SMILES Code: O=C(NC1=CC=C(CC(C)C)C=C1)NCCCN(C[C@H]2O[C@@H](N3C=C(Br)C4=C(N)N=CN=C43)[C@H](O)[C@@H]2O)C(C)C
SynonymsSGC 0946; SGC0946; SGC-0946
实验参考方法
In Vitro

In vitro activity: SGC 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.


Kinase Assay: SGC0946 is a highly potent and selective DOT1L methyltransferase inhibitor with IC50 of 0.3 nM; selectively kill mixed lineage leukaemia cells.


Cell Assay: 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.

In Vivo
Animal model
Formulation & Dosage
References

Nat Commun. 2012;3:1288.