INCB018424 Inhibitor CAS No. 941678-49-5

Cat. No.	Name	Size	Price
KI0207	INCB018424	5 mg	$179.2
	INCB018424	10 mg	$257.6
	INCB018424	25 mg	$358.4
	INCB018424	100 mg	$896

Chemical Characteristic

Product Name	INCB018424
Synonyms	Ruxolitinib
CAS No.	941678-49-5
Molecular Weight	306.37
Formula	C₁₇H₁₈N₆
Chemical Name	(betaR)-beta-Cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazole-1-propanenitrile
Smiles	n1(ncc(c1)c1c2c(ncn1)[nH]cc2)C(CC#N)C1CCCC1
Chemical Structure

Biological activities

INCB018424 is a potent and selective inhibitor of JAK1 (Janus kinase) and JAK2 with IC50 of 3.3 and 2.8 nM, respectively. However, the IC50 of INCB018424 is 428 nM against JAK3. INCB018424 inhibits interleukin-6 signaling and proliferation of JAK2^V617F+ Ba/F3 cells with IC50 of 281 and 127 nM, respectively. In primary cultures, INCB018424 preferentially suppresses erythroid progenitor colony formation (from JAK2^V617F+ polycythemia vera patients) with an IC50 of 67 nM.^[1] INCB018424 reduces the proliferation and survival of Ba/F3 cells transformed to IL3 (interleukin-3) independence by ETV6-JAK2 with an IC50 of 370 nM, compared with KG1A or Ba/F3 cells transformed by BCR-ABL1, SPBN1-FLT3 and ZMYM2-FGFR1 with IC50 of >10 µM.^[2] In a mouse model of JAK2^V617F+ myeloproliferative neoplasm (MPN), oral INCB018424 markedly reduces splenomegaly and circulating levels of inflammatory cytokines, and preferentially eliminated neoplastic cells, resulting in significantly prolonged survival without myelosuppressive or immunosuppressive effects.^[1]

Protocols

INCB018424 is dissolved in 0.2% final DMSO .^[1]

References

[1] Quint?s-Cardama A, et al. Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms. Blood. 2010, 115(15): 3109-3117. [2] Chase A, et al. Ruxolitinib as potential targeted therapy for patients with JAK2 rearrangements. Haematologica. 2012.

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