bs-60101C
[Life Science]
SGC0946 --- DOT1L inhibitor
DATASHEET
Formulation Powder
Storage: Store in dry, dark place at -20C for 1 year.
Product Information:
Molecular Weight: 618.57
Formula: C28 H40 Br N7 O4
CAS Number: 1561178-17-3
InChi Key: IQCKJUKAQJINMK-HUBRGWSESA-N
InChi: InChI=1S/C28H40BrN7O4/c1-16(2)35(12-6-11-31-27(39)34-18-9-7-17(8-10-18)28(3,4)5)14-20-22(37)23(38)26(40-20)36-13-19(29)21-24(30)32-15-33-25(21)36/h7-10,13,15-16,20,22-23,26,37-38H,6,11-12,14H2,1-5H3,(H2,30,32,33)(H2,31,34,39)/t20-,22-,23-,26-/m1/s1
Smiles: CC(C)N(C[C@H]1O[C@H]([C@H](O)[C@@H]1O)N1C=C(Br)C2=C1N=CN=C2N)CCCNC(=O)NC1C=CC(=CC=1)C(C)(C)C
Purity: 98.0
Solubility: DMSO up to 100 mM
Appearance: Solid Power.
Shelf Life: 1.0 years
Formula: C28 H40 Br N7 O4
CAS Number: 1561178-17-3
InChi Key: IQCKJUKAQJINMK-HUBRGWSESA-N
InChi: InChI=1S/C28H40BrN7O4/c1-16(2)35(12-6-11-31-27(39)34-18-9-7-17(8-10-18)28(3,4)5)14-20-22(37)23(38)26(40-20)36-13-19(29)21-24(30)32-15-33-25(21)36/h7-10,13,15-16,20,22-23,26,37-38H,6,11-12,14H2,1-5H3,(H2,30,32,33)(H2,31,34,39)/t20-,22-,23-,26-/m1/s1
Smiles: CC(C)N(C[C@H]1O[C@H]([C@H](O)[C@@H]1O)N1C=C(Br)C2=C1N=CN=C2N)CCCNC(=O)NC1C=CC(=CC=1)C(C)(C)C
Purity: 98.0
Solubility: DMSO up to 100 mM
Appearance: Solid Power.
Shelf Life: 1.0 years
Description:
SGC0946 is a highly potent and selective inhibitor of DOT1L methyltransferase. It selectively blocks binding of the cofactor, S-adenosylmethionine, to DOT1L, and inhibits the enzyme with an IC50 of 0.3 nM in a radioactive enzyme assay and is over 100-fold selective for other histone methyltransferases/HMTs. SGC0946 potently reduces H3K79 dimethylation with cellular 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. SGC0946 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.
Size: 2 mg solid, 10mg solid, 10 mM DMSO (0.323 mL2 mg solid, 10mg solid, 10 mM DMSO (0.323 mL)
Applications: Life Science()
For research use only. Not intended for diagnostic or therapeutic use.