IF 15
PMID: 40195298 ↗AZD1480
Catalog No.: GC12504Purity:>98.00%
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
10mM (in 1mL DMSO)In Stock
$62.00
1
5mgIn Stock
$56.00
1
10mgIn Stock
$88.00
1
50mgIn Stock
$260.00
1
100mgIn Stock
$450.00
1
200mgIn Stock
$600.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mM (in 1mL DMSO) | $62.00 | In Stock | 1 | |
| 5mg | $56.00 | In Stock | 1 | |
| 10mg | $88.00 | In Stock | 1 | |
| 50mg | $260.00 | In Stock | 1 | |
| 100mg | $450.00 | In Stock | 1 | |
| 200mg | $600.00 | In Stock | 1 |
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com
Citations
3 publicationsPublications from researchers using this productDescription
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.
Protocol
| 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: | |
Product Documents
Purity:>98.00%Appearance:A solid
Chemical Properties
CAS No.
935666-88-9
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
SMILES
CC1=CC(=NN1)NC2=NC(=NC=C2Cl)NC(C)C3=NC=C(C=N3)F
Molecular Formula
C14H14ClFN8
Molecular Weight
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
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
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