| Cat. No. |
Product Name |
CAS No. |
Information |
| H4190 |
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. p |
| H4189 |
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. |
| H4186 |
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. |
| H4184 |
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. |
| H4183 |
Ruxolitinib
|
941678-49-5 |
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. |
| H4171 |
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. |
| H4170 |
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. |
| H4169 |
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.
|
| H4149 |
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). |
| H4148 |
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). |
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