All Photos(2)
Synonym(s):
8-(((2r,5r)-5-Amino-1,3-dioxan-2-yl)methyl)-6-(2-chloro-4-(3-fluoropyridin-2-yl)phenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one trifluoroacetate, 8-[(trans -5-Amino-1,3-dioxan-2-yl)methyl]-6-[2-chloro-4-(3-fluoro-2-pyridinyl)phenyl]-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one trifluoroacetate
Empirical Formula (Hill Notation):
C24H22ClFN6O3 · xC2HF3O2
Recommended Products
Quality Level
Assay
≥96% (HPLC)
form
powder
storage condition
desiccated
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
Biochem/physiol Actions
MRIA9 is an ATP site-targeting, dual salt-inducible kinase (SIK1/2/3 IC50 = 55/48/22 nM; SIK2/3 IC50 = 180/127 nM by cell-based NanoBRET) & p21-activated kinase (PAK2/3 IC50 = 41/140 nM; PAK1 IC50 = 580 nM) inhibitor with excellent selectivity over other kinases. MRIA9 sensitizes ovarian cancer cells to mitotic agent paclitaxel (Pac) treatment in SKOV3 cultures (1 nM Pac plus 0.5-5 µM MRIA9) and HeLa spheroids (2 nM Pac plus 5 µM MRIA9).
Caution
Hygroscopic
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
新产品
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Roberta Tesch et al.
Journal of medicinal chemistry, 64(12), 8142-8160 (2021-06-05)
Salt-inducible kinases (SIKs) are key metabolic regulators. The imbalance in SIK function is associated with the development of diverse cancers, including breast, gastric, and ovarian cancers. Chemical tools to clarify the roles of SIK in different diseases are, however, sparse
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