Cas No. |
Product name |
1187594-09-7 |
Baricitinib (LY3009104, INCB028050) |
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Baricitinib is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Phase 3 |
941678-49-5 |
Ruxolitinib(INCB018424) |
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INCB018424 is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivity for JAK1/2 versus JAK3. |
950769-58-1 |
Quizartinib (AC220) |
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Quizartinib (AC220) is a second-generation FLT3 inhibitor for Flt3(ITD/WT) with IC50 of 1.1 nM/4.2 nM, 10-fold more selective for Flt3 than KIT, PDGFRα, PDGFRβ, RET, and CSF-... |
501919-59-1 |
NSC 74859(S3I-201) |
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S3I-201 shows potent inhibition of STAT3 DNA-binding activity with IC50 of 86 μM, and low activity towards STAT1 and STAT5. |
934353-76-1 |
ENMD-2076 |
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ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to VEGFR2/K... |
937265-83-3 |
ARRY380 |
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ARRY-380 is a potent and selective HER2 inhibitor with IC50 of 8 nM, equipotent against truncated p95-HER2, 500-fold more selective for HER2 versus EGFR. Phase 1. |
1457983-28-6 |
G-749 |
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G-749 is a novel FLT3 inhibitor that showed potent and sustained inhibition of the FLT3 wild type and mutants with IC50s of 0.4/0.6/3.5/7.5 nM for Wt Flt3/D835Y/MV4-11/Molm-1... |
1346572-63-1 |
GSK-503 |
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GSK-503 is a potent EZH2 inhibitor with potential anticancer activity. |
1401033-86-0 |
AMG 925 |
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AMG 925 is a potent and orally bioavailable dual FLT3/CDK4 inhibitor with IC50 of 1 nM and 3 nM, respectively. |
1000669-72-6 |
KW-2449 |
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KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 with IC50 of 6.6 nM, modestly potent to FGFR1, Bcr-Abl and Aurora A; little effect on PDGFRβ, IGF-1R, EGFR. |