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Request The Product List ofBone Cancer Bone Cancer

    Bone cancer is characterized by uncontrolled growth of cells of the bone. Primary bone cancer (that arises directly in the bone), is relatively rare. Different types of bone tissue give rise to different types of primary bone cancer: osteosarcoma develops from cells that form the bone and Ewing sarcoma develops from immature nerve tissue within the bone.

Cat. No. Product Name CAS No. Information
GY02421

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.

GY02113

CYT387 Mesylate

1056636-07-7

A potent and selective JAK1/JAK2 inhibitor with IC50 of 11/18 nM; shows significantly less activity against other kinases, including JAK3 (IC50=155 nM); inhibits JAK2V617F (JH1-JH2) withIC50 of 11 nM; inhibits growth of Ba/F3-JAK2V617F and HEL cells (IC50=1500 nM) or Ba/F3-MPLW515L cells (IC50=200 nM).

GY02112

CYT387 sulfate salt

1056636-06-6

A potent and selective JAK1/JAK2 inhibitor with IC50 of 11/18 nM; shows significantly less activity against other kinases, including JAK3 (IC50=155 nM); inhibits JAK2V617F (JH1-JH2) withIC50 of 11 nM; inhibits growth of Ba/F3-JAK2V617F and HEL cells (IC50=1500 nM) or Ba/F3-MPLW515L cells (IC50=200 nM).

GY04110

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.

GY01482

TG-101209

936091-14-4

TG-101209 is 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.

GY01450

BMS-911543

1271022-90-2

BMS-911543 is a potent and selective small-molecule inhibitor of JAK2 with IC50 of 1.1 nM; displays 350-, 75- and 65-fold selective to JAK1, JAK3 and TYK2, respectively; displays anti-proliferative effect on JAK2(V617F) MPNs and inhibits pSTAT5 in Ba/FJAK2V617F cells (IC50=60 nM); highly active in in vivo models and orally bioactive.

GY01230

Momelotinib

1056634-68-4

Momelotinib is a potent and selective JAK1/JAK2 inhibitor with IC50 of 11/18 nM; shows significantly less activity against other kinases, including JAK3 (IC50=155 nM); inhibits JAK2V617F (JH1-JH2) withIC50 of 11 nM; inhibits growth of Ba/F3-JAK2V617F and HEL cells (IC50=1500 nM) or Ba/F3-MPLW515L cells (IC50=200 nM).

GY01120

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.

GY01004

Ruxolitinib

941678-49-5

Ruxolitinib is 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.

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