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SML3792

Sigma-Aldrich

MRIA9 Trifluoroacetate

≥96% (HPLC)

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

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About This Item

Empirical Formula (Hill Notation):
C24H22ClFN6O3 · xC2HF3O2
Molecular Weight:
496.92 (free base basis)
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.21

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

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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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