Chemical Structure : MS2928 TFA
CAS No.:
3124729-17-2
MS2928 TFA
(MS-2928 TFA)
Catalog No.: PC-28194Not For Human Use, Lab Use Only.
MS2928 TFA is a potent and selective SETD8 covalent inhibitor, inhibits SETD8 methyltransferase activity with IC50 of 0.14 uM, covalently modifies SETD8 at Cys311.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
MS2928 TFA is a potent and selective SETD8 covalent inhibitor, inhibits SETD8 methyltransferase activity with IC50 of 0.14 uM, covalently modifies SETD8 at Cys311.
MS2928 displays excellent selectivity for SETD8 over 20 other methyltransferases.
MS2928 shows potent cellular activity, effectively reducing H4K20me1 levels and inhibiting cancer cell proliferation in SETD8-overexpressing MM cell lines, while sparing SETD8-low expressing MM cells and normal cells.
MS2928 induces significant growth inhibition of both JJN-3 and OPM-2 cells in a concentration-dependent manner, with IC50 values of 1.06 ± 0.13 and 0.54 ± 0.05 μM, respectively.
MS2928 (25 mg/kg, i.p.) effectively suppressed tumor growth in vivo in SETD8-overexpressing MM cell line xenograft mouse models.
Physicochemical Properties
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M.Wt
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526.51
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Formula
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C23H29F3N6O5
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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2-Propynamide, N-[3-[[7-(2-aminoethoxy)-6-methoxy-2-(1-pyrrolidinyl)-4-quinazolinyl]amino]propyl]-, 2,2,2-trifluoroacetate (1:1)
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References
1. He Chen, et al. J Med Chem. 2026 Feb 26;69(4):4255-4269.
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