Cat. No.: HY-10193

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AZD-1480

21 Cited Publications

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Based on 21 publication(s) in Google Scholar

AZD-1480 is an ATP-competitive inhibitor of JAK1 and JAK2 with IC₅₀s of 1.3 nM and <0.4 nM, respectively.

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Pureté: 99.74%
CAS No.: 935666-88-9
Formule: C₁₄H₁₄ClFN₈
Masse moléculaire:348.77

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

AZD-1480 Chemical Structure

CAS No.: 935666-88-9

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (21)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

AZD-1480 is an ATP-competitive inhibitor of JAK1 and JAK2 with IC₅₀s of 1.3 nM and <0.4 nM, respectively^[1].

IC₅₀ & Target^[1]

JAK2

<0.4 nM (IC₅₀)

JAK1

1.3 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform JAK :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	GI₅₀	0.06 μM Compound: 9e	Growth inhibition of mouse BA/F3 cells expressing Tel-JAK2 kinase after 48 hrs by MTS assay Growth inhibition of mouse BA/F3 cells expressing Tel-JAK2 kinase after 48 hrs by MTS assay	[PMID: 21138246]
BaF3	GI₅₀	0.7 μM Compound: 9e	Growth inhibition of mouse BA/F3 cells expressing Tel-JAK1 kinase after 48 hrs by MTS assay Growth inhibition of mouse BA/F3 cells expressing Tel-JAK1 kinase after 48 hrs by MTS assay	[PMID: 21138246]
BaF3	GI₅₀	2 μM Compound: 9e	Growth inhibition of mouse BA/F3 cells expressing Tel-Tyk2 kinase after 48 hrs by MTS assay Growth inhibition of mouse BA/F3 cells expressing Tel-Tyk2 kinase after 48 hrs by MTS assay	[PMID: 21138246]
BaF3	GI₅₀	2.1 μM Compound: 9e	Growth inhibition of mouse BA/F3 cells expressing Tel-JAK3 kinase after 48 hrs by MTS assay Growth inhibition of mouse BA/F3 cells expressing Tel-JAK3 kinase after 48 hrs by MTS assay	[PMID: 21138246]
BaF3	IC₅₀	0.046 μM Compound: 9e	Inhibition of Stat5 phosphorylation in mouse Ba/F3 cells expressing TEL-Jak2 Inhibition of Stat5 phosphorylation in mouse Ba/F3 cells expressing TEL-Jak2	[PMID: 21138246]
HEL	GI₅₀	0.39 μM Compound: 9e	Growth inhibition of human HEL cells expressing Jak2 V617F mutant after 48 hrs by MTS assay Growth inhibition of human HEL cells expressing Jak2 V617F mutant after 48 hrs by MTS assay	[PMID: 21138246]
HEL	IC₅₀	0.041 μM Compound: 9e	Inhibition of Stat5 phosphorylation in human HEL cells after 1 hr by Western blotting Inhibition of Stat5 phosphorylation in human HEL cells after 1 hr by Western blotting	[PMID: 21138246]
HEL	IC₅₀	0.08 μM Compound: 9e	Inhibition of Stat3 phosphorylation in human HEL cells after 1 hr by Western blotting Inhibition of Stat3 phosphorylation in human HEL cells after 1 hr by Western blotting	[PMID: 21138246]
HEL	IC₅₀	0.73 μM Compound: AZD1480	Antiproliferative activity against human HEL cells harboring JAK2 V617F mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HEL cells harboring JAK2 V617F mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 33689932]
MDA-MB-468	IC₅₀	5.87 μM Compound: AZD1480	Antiproliferative activity against human MDA-MB-468 cells overexpressing STAT3 assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 cells overexpressing STAT3 assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 33689932]
SET-2	GI₅₀	0.016 μM Compound: 9e	Growth inhibition of human SET2 cells expressing Jak2 V617F mutant after 48 hrs by MTS assay Growth inhibition of human SET2 cells expressing Jak2 V617F mutant after 48 hrs by MTS assay	[PMID: 21138246]

In Vitro

AZD-1480 (5μM) induces G2/M arrest and cell death by inhibiting Aurora kinases^[1].
AZD-1480 is a potent JAK2 inhibitor that can suppress growth, survival, as well as FGFR3 and STAT3 signaling and downstream targets including Cyclin D2 in human multiple myeloma cells. At low micromolar concentrations, AZD-1480 blocks cell proliferation and induces apoptosis of myeloma cell lines^[2].
AZD-1480 effectively blocks constitutive and stimulus-induced JAK1, JAK2, and STAT-3 phosphorylation in both human and murine glioma cells, and leads to a decrease in cell proliferation and induction of apoptosis^[3].
AZD-1480 is a potent, competitive small-molecule inhibitor of JAK1/2 kinase, and that it is capable of inhibiting STAT3 phosphorylation and tumor growth in a STAT3-dependent manner. AZD-1480 inhibits tumor angiogenesis and metastasis in part by affecting the tumor microenvironment^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

AZD-1480 inhibits the STAT3 phosphorylation in an xenograft model of human solid tumors and multiple myeloma^[1].
In vivo, AZD-1480 inhibits the growth of subcutaneous tumors and increases survival of mice bearing intracranial glioblastoma (GBM) tumors by inhibiting STAT-3 activity, indicating that pharmacologic inhibition of the JAK/STAT-3 pathway by AZD-1480 should be considered for study in the treatment of patients with GBM tumors^[3].
AZD-1480 blocks lung infiltration of myeloid cells and formation of pulmonary metastases in both mouse syngeneic experimental and spontaneous metastatic models. Furthermore, AZD-1480 reduces angiogenesis and metastasis in a human xenograft tumor model^[4].
AZD-1480 suppresses the growth of human solid tumor xenografts harboring persistent Stat3 activity^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 935666-88-9
Appearance Solid
Masse moléculaire 348.77
Formule C₁₄H₁₄ClFN₈
Color White to yellow
SMILES

ClC1=C(N=C(N=C1)N[C@@H](C)C2=NC=C(C=N2)F)NC3=NNC(C)=C3
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (21)

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Journal Impact Factor

Nature

Microbial metabolite drives ageing-related clonal haematopoiesis via ALPK1. [Abstract]

2025 Jun;642(8066):201-211. PMID: 40269158
Cancer Res

SMAD4 and KRAS Status Shape Cancer Cell-Stromal Crosstalk and Therapeutic Response in Pancreatic Cancer. [Abstract]

2025 Apr 15;85(8):1368-1389. PMID: 39841099
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Neuro Oncol

Tyrosine receptor kinase B is a drug target in astrocytomas. [Abstract]

2017 Jan;19(1):22-30. PMID: 27402815

AZD-1480 purchased from MedChemExpress. Usage Cited in: Neuro Oncol. 2017 Jan;19(1):22-30. [Abstract]

AZD1480 and RXDX-101 decrease pSTAT3 levels in a dose- and time-dependent manner. (A) Ink4a^-/-/Arf^-/-/NTRK2-TEL astrocytes are treated with different concentrations of AZD1480 (upper panel) or RXDX-101 (lower panel) for 1 h. (B) Cells are treated with 0.5 μM AZD1480 (upper panel) or 0.05 μM RXDX-101 (lower panel) for the indicated times. Western blot analyses are then performed with the indicated antibodies.
Leukemia

Using combination therapy to override stromal-mediated chemoresistance in mutant FLT3-positive AML: synergism between FLT3 inhibitors, dasatinib/multi-targeted inhibitors and JAK inhibitors. [Abstract]

2012 Oct;26(10):2233-44. PMID: 22469781
Cell Rep Med

Zeaxanthin augments CD8+ effector T cell function and immunotherapy efficacy. [Abstract]

2025 Sep 16;6(9):102324. PMID: 40897177
J Exp Med

EML4-ALK fusions drive lung adeno-to-squamous transition through JAK-STAT activation. [Abstract]

2024 Mar 4;221(3):e20232028. PMID: 38284990
Clin Cancer Res

STAT5A/B Blockade Sensitizes Prostate Cancer to Radiation through Inhibition of RAD51 and DNA Repair. [Abstract]

2018 Apr 15;24(8):1917-1931. PMID: 29483142

AZD-1480 purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2018 Apr 15;24(8):1917-1931. [Abstract]

Jak2 is inhibited by lentiviral expression of Jak2 shRNA or control shRNA in CWR22Pc and CWR22Rv1 cells. Alternatively, cells are treated with Jak2 inhibitors AZD1480 (0.8 μM) and INCB018424 (0.4 μM) (72 h), followed by Western blot analysis of Jak2 and active Stat5a/b.
Acta Pharmacol Sin

Inhibiting the Otub1/phosphorylated STAT3 axis for the treatment of non-small cell lung cancer. [Abstract]

2025 Jan;46(1):184-195. PMID: 39198663
Biomed Pharmacother

Effects of apigenin pretreatment against renal ischemia/reperfusion injury via activation of the JAK2/STAT3 pathway. [Abstract]

2017 Nov:95:1799-1808. PMID: 28962085

AZD-1480 purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2017 Nov:95:1799-1808. [Abstract]

The expression of Bcl-2, Bax, pro-Caspase-3 and cleaved-Caspase-3 by western blotting. Representative western blots showing the effects of apigenin and AZD1480 on Bax, Bcl-2, pro-Caspase-3 and cleaved-Caspase-3 expression levels.
Mol Cancer Ther

Enzalutamide-Induced Feed-Forward Signaling Loop Promotes Therapy-Resistant Prostate Cancer Growth Providing an Exploitable Molecular Target for Jak2 Inhibitors. [Abstract]

2020 Jan;19(1):231-246. PMID: 31548294
J Ethnopharmacol

Fu-Zheng-Tong-Luo formula promotes autophagy and alleviates idiopathic pulmonary fibrosis by controlling the Janus kinase 2/signal transducer and activator of transcription 3 pathway. [Abstract]

2023 Oct 5:314:116633. PMID: 37207878
J Biotechnol

Interferon inhibitors increase rAAV production in HEK293 cells. [Abstract]

2025 Mar:399:9-18. PMID: 39824361
J Biochem Mol Toxicol

Heme Oxygenase-1 Regulates the JAK/STAT Pathway to Inhibit Ferroptosis in Metabolic Dysfunction-Associated Steatotic Liver Disease. [Abstract]

2026 Jan;40(1):e70661. PMID: 41486516
STAR Protoc

Protocol for high-content drug screening using tumor organoids on a 384-pillar plate platform. [Abstract]

2025 Dec 1;6(4):104250. PMID: 41335519
bioRxiv

2026 Jan 22.
bioRxiv

PAIRWISE: Deep Learning-based Prediction of Effective Personalized Drug Combinations in Cancer. [Abstract]

2024 Nov 6:2024.11.04.621884. PMID: 39574568
bioRxiv

2024 Apr 30.
J Pers Med

IL4Rα and IL13Rα1 Are Involved in the Development of Human Gallbladder Cancer. [Abstract]

2022 Feb 9;12(2):249. PMID: 35207737
University of Toronto

2019 Nov.
Patent

US20180263995A1.

Solvant et solubilité

In Vitro:

DMSO : 50 mg/mL (143.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.8672 mL

14.3361 mL

28.6722 mL

5 mM

0.5734 mL

2.8672 mL

5.7344 mL

10 mM

0.2867 mL

1.4336 mL

2.8672 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (7.17 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (7.17 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (7.17 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocole

Kinase Assay^[5]

Inhibition studies of AZD1480 are performed using recombinant Jak1, Jak2, or Jak3 under buffer conditions of 50 mM HEPES pH 7.3, 1 mM DTT, 0.01% Tween-20, 50 mM/mL BSA, and 10 mM MgCl₂. Jak3 enzyme is expressed as N-terminal GST fusion in insect cells and purified by glutathione-affinity and size-exclusion chromatographies. Enzymes are assayed in the presence of AZD1480 (10 point dose response, in triplicate, from 8.3 μM to 0.3 nM in half-log dilution steps) using 1.5 μM peptide substrate (Jak1: FITC-C6-KKHTDDGYMPMSPGVA-NH2, Jak2 and Jak3: FAM-SRCtide) and screened under their respective ATP K_m (Jak1: 55 μM, Jak2: 15 μM, Jak3: 3 μM) and approximated physiological ATP concentration of 5 mM. Phosphorylated and unphosphorylated peptides are separated and quantified by a Caliper LC3000 system for calculating percent inhibition.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[4]

Renca or 786-O cells are suspended in DMEM medium with 5% FBS, and seeded in 96-well plates (5×10³ per well) to allow adhesion and then treated with DMSO or AZD1480 for 48 hours. Cell viability is determined by MTS assay. Absorbance at 490 nm is measured with Mikrotek Laborsysteme. Mouse endothelial cells and splenic CD11b+/c- myeloid cells are enriched from tumor-bearing mice,and cultured in 5% FBS RPMI-1640 medium. HUVECs are cultured on collagen 1-coated plates in complete medium. All cells are treated with DMSO and AZD1480 at various doses for 24 hours. Cell viability is determined by counting cell number manually. All the experiments are repeated 3 times.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

For subcutaneous (s.c.) tumor model, 2.5×10⁶ Renca or 786-O cells suspended in 100 μL PBS are injected into the flank of BALB/c or nude mice, respectively. When average tumor volume reaches approximately 100-150 mm³, AZD1480 or vehicle is administered by oral gavage either once a day at the dose of 50 mg/kg, or twice daily at 30 mg/kg, as indicated. Tumor size is measured by caliper every other day. For experimental lung metastasis model, 0.1×10⁶ Renca or 1×10⁶ 786-O cells suspended in 500 μL PBS are injected via tail vein to BALB/c or nude mice, respectively. Three days later, mice are orally treated with AZD1480 (50 mg/kg/d) or vehicle for 21 days for Renca tumors and 60 days for 786-O tumors respectively. For the Calu-6 model, 3×10⁶ tumor cells in matrigel are implanted s.c. into the flanks of nude mice, randomized into vehicle (twice daily, BID) and drug treatment (AZD1480, 30 mg/kg BID) groups, and dosed orally daily for 19 days. For spontaneous lung metastasis model, 2×10⁵ 4T1 cells suspended in 100 μL PBS are injected in the mammary gland of female BALB/c mice by gently penetrating the skin. AZD1480 (50 mg/kg/d) or vehicle is given orally for 21 days.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (282 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Derenzini E, et al. The JAK inhibitor AZD1480 regulates proliferation and immunity in Hodgkin lymphoma. Blood Cancer J. 2011 Dec;1(12):e46. [Content Brief]

[2]. Scuto A, et al. The novel JAK inhibitor AZD1480 blocks STAT3 and FGFR3 signaling, resulting in suppression of human myeloma cell growth and survival. Leukemia. 2011 Mar;25(3):538-50. [Content Brief]

[3]. McFarland BC, et al. Therapeutic potential of AZD1480 for the treatment of human glioblastoma. Mol Cancer Ther. 2011 Dec;10(12):2384-93. [Content Brief]

[4]. Xin H, et al. Antiangiogenic and antimetastatic activity of JAK inhibitor AZD1480. Cancer Res. 2011 Nov 1;71(21):6601-10. [Content Brief]

[5]. Hedvat M, et al. The JAK2 inhibitor AZD1480 potently blocks Stat3 signaling and oncogenesis in solid tumors. Cancer Cell. 2009 Dec 8;16(6):487-9 [Content Brief]

[6]. Ni J, et al. Tyrosine receptor kinase B is a drug target in astrocytomas. Neuro Oncol. 2017 Jan;19(1):22-30. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.8672 mL	14.3361 mL	28.6722 mL	71.6805 mL
	5 mM	0.5734 mL	2.8672 mL	5.7344 mL	14.3361 mL
	10 mM	0.2867 mL	1.4336 mL	2.8672 mL	7.1680 mL
	15 mM	0.1911 mL	0.9557 mL	1.9115 mL	4.7787 mL
	20 mM	0.1434 mL	0.7168 mL	1.4336 mL	3.5840 mL
	25 mM	0.1147 mL	0.5734 mL	1.1469 mL	2.8672 mL
	30 mM	0.0956 mL	0.4779 mL	0.9557 mL	2.3893 mL
	40 mM	0.0717 mL	0.3584 mL	0.7168 mL	1.7920 mL
	50 mM	0.0573 mL	0.2867 mL	0.5734 mL	1.4336 mL
	60 mM	0.0478 mL	0.2389 mL	0.4779 mL	1.1947 mL
	80 mM	0.0358 mL	0.1792 mL	0.3584 mL	0.8960 mL
	100 mM	0.0287 mL	0.1434 mL	0.2867 mL	0.7168 mL

Keywords

AZD-1480

21 Cited Publications

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AZD-1480

Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

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Anti-Aging Compound Library

Drug Repurposing Compound Library

Differentiation Inducing Compound Library

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Anti-Lung Cancer Compound Library

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Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) AZD-1480

Voir tous les produits spécifiques à Isoform JAK

Activité biologique

Chemical Information

Publications (21)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

AZD-1480 Related Classifications

HY-10193 Related Classifications