AZD1480 |
Catalog No.GC12504
One-Click Copy Product Info
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AZD1480 is a JAK inhibitor (JAK1: IC50 = 1.3nM; JAK2: IC50 = 0.4nM) .
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 935666-88-9
Sample solution is provided at 25 µL, 10mM.
AZD1480 is a JAK inhibitor (JAK1: IC50 = 1.3nM; JAK2: IC50 = 0.4nM) [1]. AZD1480 exerts anti-tumor effects by blocking the JAK/STAT signaling pathway and is commonly used to treat solid tumors [2-3].
In LN-17 cells, cell viability was inhibited in a dose-dependent manner after AZD1480 (0.5μM, 1μM; 72h) treatment [4]. In U251-MG and U87-MG cells, AZD1480 (1μM; 72h) inhibits constitutive STAT-3 and JAK2 activation in glioma cells [5]. In NCI-N592 cells, AZD1480 (0.3μM, 1μM, 3μM; 48h) induces G2-M cell-cycle arrest and apoptosis [6]. In CWR22Rv1 cells, AZD1480 (0-400nM; 2h) effectively reduced both ligand-induced and constitutive activation of Stat5a/b in a dose-dependent manner [7].
In Renca cell subcutaneous tumor mice model, AZD1480 (50mg/kg; po; 14d) inhibits Renca tumor growth in vivo with a reduction in tumor myeloid cell infiltration [8]. In HEK293T cell xenograft mice model, AZD1480 (30mg/kg, 50mg/kg; po; 28d) reduces angiogenesis and significantly decreases tumor volume in mouse xenograft models [9]. In MO4 cell xenograft mice model, AZD1480 (30mg/kg; po; 7d) delays tumor growth in a melanoma model while enhancing the suppressive activity of myeloid-derived suppressor cells [10].
References:
[1]. Wang SW, Hu J, Guo QH, et al. AZD1480, a JAK inhibitor, inhibits cell growth and survival of colorectal cancer via modulating the JAK2/STAT3 signaling pathway. Oncology Reports. 2014 Nov; 32(5): 1991-1998.
[2]. Suryani S, Bracken LS, Harvey RC, et al. Evaluation of the in vitro and in vivo efficacy of the JAK inhibitor AZD1480 against JAK-mutated acute lymphoblastic leukemia. Molecular cancer therapeutics. 2015 Feb 1; 14(2): 364-374.
[3]. Plimack ER, LoRusso PM, McCoon P, et al. AZD1480: a phase I study of a novel JAK2 inhibitor in solid tumors. The oncologist. 2013 Jul 1; 18(7): 819-820.
[4]. Hedvat M, Huszar D, Herrmann A, et al. The JAK2 inhibitor AZD1480 potently blocks Stat3 signaling and oncogenesis in solid tumors. Cancer cell. 2009 Dec 8; 16(6): 487-497.
[5]. McFarland BC, Ma JY, Langford CP, et al. Therapeutic potential of AZD1480 for the treatment of human glioblastoma. Molecular cancer therapeutics. 2011 Dec 1;10(12): 2384-2393.
[6]. Lee JH, Park KS, Alberobello AT, et al. The Janus kinases inhibitor AZD1480 attenuates growth of small cell lung cancers in vitro and in vivo. Clinical Cancer Research. 2013 Dec 15; 19(24): 6777-6786.
[7]. Gu L, Liao Z, Hoang DT, et al. Pharmacologic Inhibition of Jak2–Stat5 Signaling By Jak2 Inhibitor AZD1480 Potently Suppresses Growth of Both Primary and Castrate-Resistant Prostate Cancer. Clinical Cancer Research. 2013 Oct 15; 19(20): 5658-5674.
[8]. Xin H, Herrmann A, Reckamp K, et al. Antiangiogenic and antimetastatic activity of JAK inhibitor AZD1480. Cancer research. 2011 Nov 1; 71(21): 6601-6610.
[9]. Murakami T, Takigawa N, Ninomiya T, et al. Effect of AZD1480 in an epidermal growth factor receptor-driven lung cancer model. Lung cancer. 2014 Jan 1; 83(1): 30-36.
[10]. Maenhout SK, Du Four S, Corthals J, et al. AZD1480 delays tumor growth in a melanoma model while enhancing the suppressive activity of myeloid-derived suppressor cells. Oncotarget. 2014 Jul 25; 5(16): 6801.
| Cell experiment [1]: | |
Cell lines | LN-17 cells |
Preparation Method | LN-17 cells (5 × 103) were plated in 96-well plates in quintuplicate in RPMI plus 10% charcoal-stripped FBS and allowed to attach for 24h prior to the addition of DMSO or AZD1480 to the culture medium. After 72h, 20μL/well of 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium/phenazine ethosulfate solution was added. After incubation (1h, 37℃, 5% CO2 atmosphere), absorbance at 490nm was recorded by using an ELISA plate reader. |
Reaction Conditions | 0.5μM, 1μM; 72h |
Applications | After AZD1480 treatment, LN-17 cell viability was inhibited in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Renca cell subcutaneous tumor mice model |
Preparation Method | For subcutaneous tumor model, 2.5 × 106 Renca cells suspended in 100μL PBS were injected into the flank of nude mice, respectively. When average tumor volume reached approximately 100 to 150mm3, AZD1480 or vehicle was administered by oral gavage either once a day at the dose of 50mg/kg, as indicated. Tumor size was measured by caliper every other day. |
Dosage form | 50mg/kg; po; 14d |
Applications | AZD1480 inhibits Renca tumor growth in vivo with a reduction in tumor myeloid cell infiltration. |
References: | |
| Cas No. | 935666-88-9 | SDF | |
| Chemical Name | 5-chloro-2-N-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-4-N-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine | ||
| Canonical SMILES | CC1=CC(=NN1)NC2=NC(=NC=C2Cl)NC(C)C3=NC=C(C=N3)F | ||
| Formula | C14H14ClFN8 | M.Wt | 348.77 |
| Solubility | ≥ 93.8 mg/mL in DMSO, ≥ 4.57 mg/mL in EtOH with ultrasonic and warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8672 mL | 14.3361 mL | 28.6722 mL |
| 5 mM | 573.4 μL | 2.8672 mL | 5.7344 mL |
| 10 mM | 286.7 μL | 1.4336 mL | 2.8672 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)