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DGY-06-116

Chemical Structure : DGY-06-116

CAS No.: 2556836-50-9

DGY-06-116 (SRC inhibitor 15a)

Catalog No.: PC-72224Not For Human Use, Lab Use Only.

DGY-06-116 (SRC inhibitor 15a) is a potent, selective, covalent Src inhibitor (biochemical IC50=3 nM) that taregrs a P-Loop cysteine (Cys277).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

DGY-06-116 (SRC inhibitor 15a) is a potent, selective, covalent Src inhibitor (biochemical IC50=3 nM) that taregrs a P-Loop cysteine (Cys277).
BTK, ABL, and most SFK family members such as HCK, BLK, LCK, and YES1 were the main off-targets as confirmed with low nanomolar biochemical IC50s.
DGY-06-116 demonstrated potent antiproliferative effects in lung and breast cancer cell lines (H1957 GI50=0.3 uM).
DGY-06-116 inhibited p-SRCY416 signaling in both H1975 and HCC827 cells at 1 uM.
DGY-06-116 inhibited p-SRCY416 at 2 and 4 h postdosing in spleen tissue samples from C57B6 mice.

Physicochemical Properties

M.Wt 597.12
Formula C32H33ClN8O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-((2-Acrylamidophenyl)amino)-N-(2-chloro-6-methylphenyl)-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidine-5-carboxamide

References

1. Guangyan Du, et al. J Med Chem. 2020 Feb 27;63(4):1624-1641.

2. Gurbani D, et al. Front Mol Biosci. 2020 May 19;7:81.

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