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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
27 Results for "
V617F
" in MedChemExpress (MCE) Product Catalog:
Products (27)
27 Results for "V617F" in MCE Product Catalog:
56
56 Publications Verification
Synonyms: TG-101348; SAR 302503
Fedratinib (TG-101348) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib induces cancer cell apoptosis and has the potential for myeloproliferative disorders research .
56
56 Publications Verification
Synonyms: TG-101348 hydrochloride hydrate; SAR 302503 hydrochloride hydrate
Fedratinib hydrochloride hydrate (TG-101348 hydrochloride hydrate) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib hydrochloride hydrate shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib hydrochloride hydrate induces cancer cell apoptosis and has the potential for myeloproliferative disorders research .
8
8 Cited Publications
XL019?is a potent, orally active, and selective JAK2 inhibitor, with IC50s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2 .
5
5 Cited Publications
TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET with IC50 of 25 nM and 17 nM, appr 30-fold selective for JAK2 than JAK3, and sensitive to JAK2V617F and MPLW515L/K mutations.
4
4 Cited Publications
Synonyms: JAK2 Inhibitor V; Z3
NSC 42834 (JAK2 Inhibitor V), a novel specific inhibitor of Jak2, inhibits Jak2-V617F and Jak2-WT autophosphorylation in a dose-dependent manner but was not cytotoxic to cells at concentrations that inhibited kinase activity.
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ZT55 is an orally active and highly-selective JAK2 inhibitor with an IC50 value of 0.031 μM. ZT55 inhibits the proliferation of JAK2 V617F-expressing HEL cell lines and induces apoptosis and cycle arrest. ZT-55 also effectively inhibits the growth of HEL xenograft tumours in a mice model. ZT-55 can be used in studies of myeloproliferative neoplasms, polycythemia vera and primary thrombocythemia .
JAK2-IN-7 is a selective JAK2 inhibitor with IC50s of 3, 11.7, and 41 nM for JAK2, SET-2, and Ba/F3 V617F cells, respectively. JAK2-IN-7 possesses >14-fold selectivity over JAK1, JAK3, FLT3. JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase and induces tumor cellapoptosis. Antitumor activities .
Cat. No.: HY-169326S
CAS No.: 3057053-17-2
Cat. No.: HY-161684
CAS No.: 3035735-18-0
Cat. No.: HY-164393
CAS No.: 1035199-04-2
ON044580 is a non–ATP-competitive JAK2 and BCR-ABL kinases inhibitor. ON044580 inhibits wild-type (WT) and V617F mutant JAK2 with IC50 values of 1.23 μM, 1.09 μM, respectively. ON044580 also inhibits both WT and T315I mutant BCR-ABL kinases., ON044580 blocks the IL-3–mediated phosphorylation of JAK2 and STAT5, induces apoptosis in Imatinib (HY-15463)-resistant chronic myeloid leukemia (CML). ON044580 can be used for the study of CML, myelodysplasia (MDS) and other myeloproliferative neoplasms .
Cat. No.: HY-10409R
CAS No.: 936091-26-8
Synonyms: TG-101348 (Standard); SAR 302503 (Standard)
Target:
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Fedratinib (Standard) is the analytical standard of Fedratinib. This product is intended for research and analytical applications. Fedratinib (TG-101348) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib induces cancer cell apoptosis and has the potential for myeloproliferative disorders research .
Cat. No.: HY-160919
CAS No.: 2982846-48-8
JAK2-IN-16 (Compound Example 4) is a JAK2 V617F inhibitor. JAK2-IN-16 can be used for the research of cancer .
Cat. No.: HY-188001
CAS No.: 3057053-13-8
JAK2-IN-22 is a bicyclic urea compound with potent binding inhibitory activity against wild-type and V617F mutant JH2 kinases (IC50 ≤ 10 nM). JAK2-IN-22 can be used in research related to various diseases including cancer .
Cat. No.: HY-189580
CAS No.: 3047885-27-5
JAK2-IN-25 is a JAK2 inhibitor with an EC50 of ≤ 0.01 μM. JAK2-IN-25 exhibits antiproliferative activity against cells expressing JAK2 V617F. JAK2-IN-25 can be used for research on myeloproliferative diseases .
Cat. No.: HY-136734
CAS No.: 1110502-30-1
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Research Areas:
JAK2-IN-5 (Compound 13) is a selective JAK kinase inhibitor, with an IC50 of 0.078 μM against JAK-2 and an IC50 of 0.206 μM against JAK-2 V617F. JAK2-IN-5 can be used for the research of myeloproliferative disorders .
Cat. No.: HY-188002
CAS No.: 3057053-16-1
JAK2-IN-23 is a highly selective JH2-binding JAK2 inhibitor, with an IC50 ≤ 10 nM for binding to both wild-type and V617F-mutated JH2. JAK2-IN-23 can be used in studies of JAK2-related diseases, such as cancer .
Cat. No.: HY-189581
CAS No.: 3047885-19-5
JAK2-IN-26 is a JAK2 inhibitor with an EC50 greater than 0.01 μM and less than or equal to 0.05 μM. JAK2-IN-26 exhibits antiproliferative activity against cells expressing JAK2 V617F. JAK2-IN-26 can be used for research on myeloproliferative disorders .
Cat. No.: HY-180561
CAS No.: 3076807-15-0
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Research Areas:
WWQ-03-012 is a selective DESI2 inhibitor with an IC50 of 47.3 nM. WWQ-03-012 binds covalently to DESI2, blocks its enzymatic activity, and inhibits DESI2-mediated deSUMOylation, deubiquitination and stabilization of mutant JAK2, thereby promoting the complete degradation of mutant JAK2 via the intracellular ubiquitin-proteasome system and inducing apoptosis, while exerting no significant effect on wild-type JAK2. WWQ-03-012 can be used for research on myeloproliferative neoplasms (MPN) and secondary acute myeloid leukemia (sAML), especially for hematological malignancies carrying the JAK2-V617F mutation and those resistant to Ruxolitinib (HY-50856) .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
