Our laboratory has not validated this product for use on human JAK. However, based on the provided citation, the inhibitor appears to demonstrate effective activity on human cells as well. The study titled "Anti-adult T‑cell leukemia/lymphoma activity of cerdulatinib, a dual SYK/JAK kinase inhibitor" published in Int J Oncol. 2018 Oct;53(4):1681-1690 (PMID: 30066853) supports this observation.
420097
JAK Inhibitor I
InSolution, ≥98%
Synonim(y):
InSolution JAK Inhibitor I, 2-(1,1-Dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, P6, Pyridone 6, DBI, JAK1 Inhibitor I, JAK2 Inhibitor I, JAK3 Inhibitor X
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500 μG
628,00 zł
628,00 zł
Dostępny w magazynieSzczegóły
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500 μG
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About This Item
Wzór empiryczny (zapis Hilla):
C18H16FN3O
Numer CAS:
Masa cząsteczkowa:
309.34
Numer MDL:
Kod UNSPSC:
12352200
NACRES:
NA.77
628,00 zł
Dostępny w magazynieSzczegóły
Polecane produkty
Poziom jakości
Próba
≥98% (HPLC)
Formularz
liquid
producent / nazwa handlowa
Calbiochem®
warunki przechowywania
OK to freeze
desiccated (hygroscopic)
protect from light
Warunki transportu
wet ice
temp. przechowywania
2-8°C
ciąg SMILES
Fc1cc2c(c3[nH]c(nc3c4c2c(ncc4)O)C(C)(C)C)cc1
InChI
1S/C18H16FN3O/c1-18(2,3)17-21-14-10-5-4-9(19)8-12(10)13-11(15(14)22-17)6-7-20-16(13)23/h4-8H,1-3H3,(H,20,23)(H,21,22)
Klucz InChI
VNDWQCSOSCCWIP-UHFFFAOYSA-N
Opis ogólny
A potent inhibitor of Janus Protein tyrosine Kinases (JAKs). Displays potent inhibitory activity against JAK1 (IC50 = 15 nM for murine JAK1), JAK2 IC50 = 1 nM), JAK3 (Ki = 5 nM), and Tyk2 (IC50 = 1 nM). It inhibits other kinases only at much higher concentrations. Also inhibits IL-2- and IL-4-dependent proliferation of CTLL cells and blocks the phosphorylation of STAT5.
Działania biochem./fizjol.
Cell permeable: yes
Primary Target
murine JAK1
murine JAK1
Product competes with ATP.
Reversible: yes
Target IC50: 15 nM, 1 nM against murine JAK1 and JAK2, respectively; 1 nM against Tyk2
Target Ki: 5 nM against JAK3
Opakowanie
Packaged under inert gas
Ostrzeżenie
Toxicity: Irritant (B)
Postać fizyczna
A 10 mM (500 µg/162 µl) solution of JAK Inhibitor I (Cat. No. 420099) in DMSO.
Rekonstytucja
Following initial use, aliquot and refrigerate (4°C).
Inne uwagi
Thompson, J.E., et al. 2002. Bioorg. Med. Chem. Lett.12, 1219.
Informacje prawne
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
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Kod klasy składowania
10 - Combustible liquids
Klasa zagrożenia wodnego (WGK)
WGK 2
Temperatura zapłonu (°F)
188.6 °F - closed cup - (Dimethylsulfoxide)
Temperatura zapłonu (°C)
87 °C - closed cup - (Dimethylsulfoxide)
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Can the InSolution JAK Inhibitor I - CAS 457081-03-7 - Calbiochem also target human JAK, considering that its primary target is stated as murine? I am in search of an inhibitor for human JAK.
1 answer-
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