AZD 1480
- Product Name
- AZD 1480
- CAS No.
- 935666-88-9
- Chemical Name
- AZD 1480
- Synonyms
- AZD 1480;AZD1480, >=98%;AZD1480 ，S2162;AZD-1480;AZD 1480;AZD-1480, 10 mM in DMSO;AZD1480;AZD1480;AZD 1480;AZD1480, 98%, a novel ATP-competitive JAK2 inhibitor;(S)-5-Chloro-N2-(1-(5-fluoropyrimidin-2-yl)ethyl)-N4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-;(S)-5-chloro-N2-(1-(5-fluoropyrimidin-2-yl)ethyl)-N4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamin;(S)-5-chloro-N2-(1-(5-fluoropyriMidin-2-yl)ethyl)-N4-(5-Methyl-1H-pyrazol-3-yl)pyriMidine-2,4-diaMine
- CBNumber
- CB92509980
- Molecular Formula
- C14H14ClFN8
- Formula Weight
- 348.77
- MOL File
- 935666-88-9.mol
AZD 1480 Property
- Melting point:
- >205°C (dec.)
- Boiling point:
- 575.2±60.0 °C(Predicted)
- Density
- 1.517
- storage temp.
- -20°C
- solubility
- Chloroform (Slightly, Heated), DMSO (Slightly, Heated), Methanol (Slightly, Heat
- form
- powder
- pka
- 13.73±0.10(Predicted)
- color
- white to beige
- InChI
- InChI=1S/C14H14ClFN8/c1-7-3-11(24-23-7)21-13-10(15)6-19-14(22-13)20-8(2)12-17-4-9(16)5-18-12/h3-6,8H,1-2H3,(H3,19,20,21,22,23,24)/t8-/m0/s1
- InChIKey
- PDOQBOJDRPLBQU-QMMMGPOBSA-N
- SMILES
- C1(N[C@H](C2=NC=C(F)C=N2)C)=NC=C(Cl)C(NC2C=C(C)NN=2)=N1
Safety
- HS Code
- 29335990
N-Bromosuccinimide Price
- Product number
- SML1505
- Product name
- AZD1480
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $131.1
- Updated
- 2025/07/31
- Product number
- SML1505
- Product name
- AZD1480
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $558
- Updated
- 2025/07/31
- Product number
- 10702
- Product name
- AZD1480
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $37
- Updated
- 2024/03/01
- Product number
- 10702
- Product name
- AZD1480
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $116
- Updated
- 2024/03/01
- Product number
- 10702
- Product name
- AZD1480
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $195
- Updated
- 2024/03/01
AZD 1480 Chemical Properties,Usage,Production
Uses
AZD1480 has been used as an inhibitor of janus kinase 2 (JAK2) and signal transducer and activator of transcription 3 (STAT3) in an in vitro cell model of upper gastrointestinal adenocarcinoma. It has also been used in combination with bortezomib to study tumor-associated macrophage-mediated survival of myeloma cells.
Biological Activity
AZD1480 is a novel small-molecule JAK inhibitor. It is able to block cell proliferation and induce apoptosis of myeloma cell lines. It can effectively inhibit tumor angiogenesis and metastasis mediated by STAT3 in stromal cells as well as tumor cells. AZD1480 has broad efficacy on a wider variety of myeloma cells, such as RPMI 8226, OPM-2, NCI-H929, Kms.18, MM1.S and IM-9, as well as primary myeloma cells. AZD1480 induces cell death of Kms.11 cells grown in the presence of HS-5 bone marrow (BM)-derived stromal cells and inhibits tumor growth in a Kms.11 xenograft mouse model, accompanied with inhibition of phospho-FGFR3, phospho-JAK2, phospho-STAT3 and Cyclin D2 levels. AZD1480 also demonstrates important Jak2 selectivity over Jak3, in particular at high ATP concentrations and marginal selectivity over Jak1 at Km ATP.
Biochem/physiol Actions
AZD1480 is an orally active, potent and selective inhibitor of Janus kinases JAK1 and JAK 2 with selectivity for JAK2 as evidenced by IC50 values of 1.3 nM for JAK1 and <0.4 nM for JAK2 in enzyme assays. AZD1480 inhibits endogenous as well as IL-6 induced STAT3 activation. AZD1480 reduces myeloid cell-mediated angiogenesis and metastasis. AZD1489 is an effective anticancer agent in bot adult and pediatric human tumors.
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].
IC 50
JAK2: <0.4 nM (IC50); JAK1: 1.3 nM (IC50)
storage
Store at -20°C
AZD 1480 Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from AZD 1480 manufacturers
- Product
- 5-Chloro-N2-[(1S)-1-(5-fluoro-2-pyrimidinyl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)-2,4-pyrimidinediamine 935666-88-9
- Price
- US $1.00/KG
- Min. Order
- 1G
- Purity
- 98%
- Supply Ability
- 100KG
- Release date
- 2018-08-21