AZ 960 - 10mM in DMSO, high purity , CAS No.905586-69-8(DMSO)

Item Number
A409099
Grouped product items
SKUSizeAvailabilityPrice Qty
A409099-1ml
1ml
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$470.90

JAK2 Selective Inhibitors

Basic Description

Specifications & PurityMoligand™, 10mM in DMSO
Biochemical and Physiological MechanismsAZ 960 is a novel ATP competitive JAK2 inhibitor with IC50 and Ki of <3 nM and 0.45 nM, 3-fold selectivity of AZ960 for JAK2 over JAK3. AZ 960 induces apoptosis and growth arrest.
Storage TempStore at -80°C
Shipped InIce chest + Ice pads
GradeMoligand™
Product Description

Information

AZ 960 is a novel ATP competitiveJAK2inhibitor withIC50andKiof <3 nM and 0.45 nM, 3-fold selectivity of AZ960 for JAK2 over JAK3. AZ 960 inducesapoptosisand growth arrest.
In vitro

AZ960 also inhibits many kinases less than 50% at a concentration of 0.1 μM such as JAK3 (IC50=9 nM), TrkA, Aurora, and ARK5. In cells, AZ 960 inhibits the phosphorylation of STAT5 in TEL-JAK2 cells with an average IC50 of 15 nM and exhibits 15-30 -fold sensitivity for TEL-JAK2-driven STAT5 phosphorylation compared with cell lines driven by other JAK kinase family members (TEL-JAK1, -JAK3, and -TYK2). AZ 960 shows potent activity in inhibiting the proliferation of the TEL-JAK2, -JAK1, -JAK3, and -Tyk2 cell lines with GI50 values of 25 nM, 230 nM, 279 nM, and 214 nM, respectively. Moreover, AZ 960 also potently inhibits SET-2 cell proliferation with an average GI50 of 33 nM by reducing both STAT3 and STAT5 phosphorylation levels. AZ 960 causes growth arrest and apoptosis of human T-cell lymphotropic virus type 1, HTLV-1pe 1, HTLV-1LV-1osis of human T-cSET-2 cell proliferation witBcl-xL by small interfering RNA potentiates anti-proliferative effects of AZ 960 in MT-1 cells. A recent study shows that AZ 960 leads to significant inhibition of the clonogenic growth and induction of apoptosis of freshly isolated AML cells from patients.

In vivo


Cell Data

cell lines:

Concentrations:0.016-10 μM

Incubation Time:48-72 hours

Powder Purity:≥99%

Product Properties

Ki DataJAK2, Ki: 0.45 nM

Associated Targets(Human)

JAK3 Tclin Tyrosine-protein kinase JAK3 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
JAK2 Tclin Tyrosine-protein kinase JAK2 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

Canonical SMILES CC(NC1=NC(=C(F)C=C1C#N)NC2=N[NH]C(=C2)C)C3=CC=C(F)C=C3
Molecular Weight 354.36

Certificates

Certificate of Analysis(COA)

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Chemical and Physical Properties

SolubilitySolubility (25°C) In vitro DMSO: 44 mg/mL (197.86 mM);    

Related Documents

Solution Calculators