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Purity: ≥98%
AZ 960 (AZ-960) is a novel, potent, selective and ATP competitive JAK2 (janus kinase) inhibitor with potential antitumor activity. It inhibits JAK2 with an IC50 and Ki of<3 nM and 0.45 nM, and displays 3-fold selectivity for JAK2 over JAK3. It shows potent in vitro antiproliferative activity and high in vivo antitumor efficacy. In recent studies, AZ960 demonstrates potential anti-cancer activity against adult T-cell leukemia (ATL), an aggressive malignancy of CD4+ T lymphocytes, by effectively inducing growth arrest and apoptosis in human T-cell lumphotropic virus type 1 (HTLV-1) infected T cells.
| ln Vitro |
Jak2 kinase is inhibited by AZ960 at a Ki of 0.45 nM. Z960 has significantly less activity against TYK2, Jak1, and 3. AZ960 has an IC50 of about 0.1 μM and is active against various kinases, including as FAK, TrkA, and Aurora-A. In human T-cell lymphotropic virus type 1, HTLV-1-infected T cells (MT-1 and MT-2), AZ960 efficiently induces growth arrest and death while downregulating the phosphorylated versions of Jak2 and Bcl-2 family proteins, including Bcl-2 and Mcl-1[2]. In recently isolated acute myeloid leukemia cells, AZ960 efficiently suppresses clonal proliferation and triggers apoptosis, which is linked to caspase 3 cleavage and downregulation of the anti-apoptotic Bcl-xL protein [1]. The AZ960 Ki for T. The value of TbERK8, or Brucei extracellular signal-regulated kinase 8, is 1.25 μM. With an IC50 of 120 nM, it inhibits TbERK8[3].
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| References |
[1]. Ikezoe T, et al. Expression of p-JAK2 predicts clinical outcome and is a potential molecular target of acute myelogenous leukemia. Int J Cancer. 2011 Nov 15;129(10):2512-21.
[2]. Gozgit JM, et al. Effects of the JAK2 inhibitor, AZ960, on Pim/BAD/BCL-xL survival signaling in the human JAK2 V617F cell line SET-2. J Biol Chem. 2008 Nov 21;283(47):32334-43. [3]. Yang J, et al. AZ960, a novel Jak2 inhibitor, induces growth arrest and apoptosis in adult T-cell leukemia cells. Mol Cancer Ther. 2010 Dec;9(12):3386-95. [4]. Valenciano AL, et al. Discovery and antiparasitic activity of AZ960 as a Trypanosoma brucei ERK8 inhibitor. Bioorg Med Chem. 2016 Oct 1;24(19):4647-51 |
| Molecular Formula |
C18H16F2N6
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| Molecular Weight |
354.36
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| CAS # |
905586-69-8
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| SMILES |
FC1C([H])=C(C#N)C(=NC=1N([H])C1C([H])=C(C([H])([H])[H])N([H])N=1)N([H])[C@@]([H])(C([H])([H])[H])C1C([H])=C([H])C(=C([H])C=1[H])F
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.05 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.05 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8220 mL | 14.1099 mL | 28.2199 mL | |
| 5 mM | 0.5644 mL | 2.8220 mL | 5.6440 mL | |
| 10 mM | 0.2822 mL | 1.4110 mL | 2.8220 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02768207 | Completed | Drug: Cobimetinib Drug: Vemurafenib |
Metastatic Melanoma | Hoffmann-La Roche | May 23, 2016 | Phase 2 |
| NCT01667419 | Completed Has Results |
Drug: Vemurafenib Drug: Placebo |
Melanoma | Hoffmann-La Roche | September 24, 2012 | Phase 3 |
| NCT01307397 | Completed Has Results |
Drug: Vemurafenib | Malignant Melanoma | Hoffmann-La Roche | March 1, 2011 | Phase 3 |
| NCT01909453 | Active, not recruiting Has Results |
Drug: LGX818 Drug: MEK162 |
Melanoma | Pfizer | December 13, 2013 | Phase 3 |
AZ960 inhibits the growth of HTLV-1–infected T cells and freshly isolated ATL cells.Mol Cancer Ther.2010 Dec;9(12):3386-95. |
The levels of Bcl-2 family. A, Western blot analysis.Mol Cancer Ther.2010 Dec;9(12):3386-95. |
Knockdown of Bcl-xL by siRNA sensitizes MT-1 cells to AZ960-induced apoptosis.Mol Cancer Ther.2010 Dec;9(12):3386-95. |
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