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Cat. No. Product Name CAS No. Information
PC-45664

NS-018 hydrochloride

1239358-85-0

NS-018 hydrochloride (NS018, Ilginatinib) is a potent and highly selective JAK2 inhibitor (IC50=0.72 nM); displays 30-50-fold greater selectivity for JAK2 over JAK1, JAK3 and Tyk2; also inhibits Src family kinases(Src, Fyn); shows effective in mouse Ba/F3-JAK2V617F disease model.

Bone Cancer

Phase 2 Clinical

PC-45663

NS-018

1239358-86-1

NS-018 (NS018, Ilginatinib) is a potent and highly selective JAK2 inhibitor (IC50=0.72 nM); displays 30-50-fold greater selectivity for JAK2 over JAK1, JAK3 and Tyk2; also inhibits Src family kinases(Src, Fyn); shows effective in mouse Ba/F3-JAK2V617F disease model.

Bone Cancer

Phase 2 Clinical

PC-45662

NS-018 maleate

1354799-87-3

NS-018 maleate (NS018, Ilginatinib) is a potent and highly selective JAK2 inhibitor (IC50=0.72 nM); displays 30-50-fold greater selectivity for JAK2 over JAK1, JAK3 and Tyk2; also inhibits Src family kinases(Src, Fyn); shows effective in mouse Ba/F3-JAK2V617F disease model.

Bone Cancer

Phase 2 Clinical

PC-42569

TG-101348

936091-26-8

TG-101348 (Fedratinib, SAR302503) is a potent, selective JAK2 inhibitor with IC50 of 3 nM for both wt JAK2 and JAK2 V617F; also inhibits FLT3 (IC50=15 nM) and RET (IC50=48 nM) kinases, weakly inhibits JAK3 (IC50=168 nM), >35-fold selectivity over JAK1/3 and Tyk2; shows therapeutic efficacy in a murine model of myeloproliferative disease induced by the JAK2V617F mutation; also potently inhibits BRD4 with Kd of 168 nM.

Bone Cancer

Phase 3 Clinical

PC-42570

TG-101209

936091-14-4 A potent, selective, orally bioavailable JAK2 inhibitor with IC50 of 6 nM; also inhibits FLT3 (IC50=25 nM) and RET (IC50=17 nM) kinases, weakly inhibits JAK3 (IC50=168 nM); inhibits growth of Ba/F3 cells expressing JAK2V617F or MPLW515L mutations with IC50 of 200 nM, induces cell cycle arrest and apoptosis, and inhibits phosphorylation of JAK2V617F, STAT5 and STAT3; attenuates myelofibrosis in murine model of JAK2V617F-induced polycythemia vera; also potently inhibits BRD4 with Kd of 123 nM.

Bone Cancer

Preclinical

PC-45875

Ruxolitinib sulfate

1092939-16-6 A potent, selective, orally active JAK1/JAK2 inhibitor with IC50 of 3.3/2.8 nM, respectively; displays modest selectivity against Tyk2 (6-fold) and marked selectivity (>130-fold) against JAK3; inhibits IL-6 signaling (IC50=281 nM), and proliferation of JAK2V617F(+) Ba/F3 cells (IC50=127 nM); suppresses erythroid progenitor colony formation from JAK2V617F(+) polycythemia vera patients (IC50=67 nM) in primary cultures; markedly reduces level of inflammatory cytokines, and preferentially eliminates neoplastic cells in a mouse model of JAK2V617F(+) MPN.

Bone Cancer

Approved

PC-45874

Ruxolitinib phosphate

1092939-17-7 A potent, selective, orally active JAK1/JAK2 inhibitor with IC50 of 3.3/2.8 nM, respectively; displays modest selectivity against Tyk2 (6-fold) and marked selectivity (>130-fold) against JAK3; inhibits IL-6 signaling (IC50=281 nM), and proliferation of JAK2V617F(+) Ba/F3 cells (IC50=127 nM); suppresses erythroid progenitor colony formation from JAK2V617F(+) polycythemia vera patients (IC50=67 nM) in primary cultures; markedly reduces level of inflammatory cytokines, and preferentially eliminates neoplastic cells in a mouse model of JAK2V617F(+) MPN.

Bone Cancer

Approved

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