Emavusertib (CA-4948) | IRAK4 inhibitor

Chemical Structure : CA-4948

CAS No.: 1801344-14-8

CA-4948 (Emavusertib, CA4948, AU-4948, AU4948)

Catalog No.: PC-50002Not For Human Use, Lab Use Only.

Emavusertib (CA-4948) is a potent, selective and orally active IRAK4 inhibitor with IC50 of 31.7 nM.

Packing	Price	Stock
5 mg	$58	In stock
10 mg	$88	In stock
25 mg	$138	In stock
50 mg	$228	In stock
100 mg	$378	In stock
250 mg		Get quote

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Biological Activity

Emavusertib (CA-4948) is a potent, selective and orally active IRAK4 inhibitor with IC50 of 31.7 nM.

Emavusertib (CA-4948) exhibits significant activity against a handful of other kinases such as CLK1, CLK2, CLK4, FLT3, DYRK1A, DYRK1B, TrkA, TrkB, Haspin, and NEK11 in a panel of a broad kinome panel (329 kinases).

Emavusertib (CA-4948) showed good modulation of IL6 in human whole blood assayand pIRAK1 modulation (IC50 of 270 nM) in MV4-11 cell-line.

Emavusertib (CA-4948) demonstrated moderate potency in OCI-Ly10 (IC50 = 1.5 μM) harboring MYD88 mutation in cellular growth inhibition assay in a short panel of lymphoma cell lines.

Emavusertib (CA-4948) showed >90% tumor growth inhibition in relevant tumor models with excellent correlation with in vivo PD modulation.

Physicochemical Properties

M.Wt	491.508
Formula	C24H25N7O5
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	Room temperature in continental US; may vary elsewhere
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-[5-[(3R)-3-Hydroxy-1-pyrrolidinyl]-2-(4-morpholinyl)oxazolo[4,5-b]pyridin-6-yl]-2-(2-methyl-4-pyridinyl)-4-oxazolecarboxamide

References

1. Robert Booher, et al. 1534 Combination of IRAK4 Inhibitor CA-4948 with BCL2 Inhibitor Venetoclax Induces Tumor Regression in an ABC-DLBCL Xenograft Model. Bldg A, Lvl 1, Hall A2 (Georgia World Congress Center).
2. Gummadi VR, et al. ACS Med Chem Lett. 2020 Oct 14;11(12):2374-2381.
3. Zhang S, et al. Front Immunol. 2021 Mar 9;12:637659.

CA-4948 (Emavusertib, CA4948, AU-4948, AU4948)

Biological Activity

Physicochemical Properties

References

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