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AZD1480,JAK2抑制剂, 酪氨酸蛋白激酶 JAK2 抑制剂

AZD1480,JAK2抑制剂, 酪氨酸蛋白激酶 JAK2 抑制剂

强效选择性JAK2抑制剂

规格或纯度: ≥98%

CAS编号: 935666-88-9
分子式: C₁₄H₁₄ClFN₈
分子量: 348.77
PubChem编号: 16659841

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货号 (SKU)	包装规格	是否现货
A126326-1mg	1mg	现货
A126326-5mg	5mg	现货
A126326-10mg	10mg	现货
A126326-25mg	25mg	现货
A126326-50mg	50mg	现货
A126326-100mg	100mg	现货

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基本描述

英文别名	AZD1480\|935666-88-9\|AZD-1480\|(S)-5-chloro-N2-(1-(5-fluoropyrimidin-2-yl)ethyl)-N4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine\|AZD 1480\|UNII-KL2Z2TLF01\|C14H14ClFN8\|KL2Z2TLF01\|CHEMBL1231124\|5-Chloro-N2-[(1s)-1-(5-Fluoropyrimidin-2-Yl)ethyl]-N4-(5-Methy
规格或纯度	≥98%
英文名称	AZD1480
生化机理	AZD1480 demonstrated significant immunoregulatory effects by downregulating T-helper 2 cytokines and chemokines, including IL-13 and thymus- and activation-regulated chemokine, and the surface expression of the immunosuppressive programmed death ligands 1 and 2. Higher concentrations of AZD1480 (5μ) induced G2/M arrest and cell death by inhibiting Aurora kinases.Novel, potent and selective small-molecule JAK2 inhibitor (IC 50 < 3 nM). \xa0It can effectively inhibit tumor angiogenesis and metastasis mediated by STAT3 in stromal cells as well as tumor cells. Also demonstrates >50-fold selectivity for JAK2 over JAK3
储存温度	-20°C储存
运输条件	超低温冰袋运输
备注	有毒，请参考SDS，以获取更多信息。需要更多有关溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。
产品介绍	AZD1480是ATP竞争性JAK2抑制剂，IC50为0.26 nM，对JAK1抑制性较弱。An inhibitor of JAK2 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.

产品属性

ALogP	2.4

名称和标识符

PubChem SID	488199394
PubChem SID url	https://pubchem.ncbi.nlm.nih.gov/substance/488199394
IUPAC Name	5-chloro-2-N-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-4-N-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine
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
InChi Key	PDOQBOJDRPLBQU-QMMMGPOBSA-N
Canonical SMILES	CC1=CC(=NN1)NC2=NC(=NC=C2Cl)NC(C)C3=NC=C(C=N3)F
Isomeric SMILES	CC1=CC(=NN1)NC2=NC(=NC=C2Cl)N[C@@H](C)C3=NC=C(C=N3)F
PubChem CID	16659841
分子量	348.77

数据库链接

PubChem CID	16659841
ChEMBL Ligand	CHEMBL1231124
CAS Registry No.	935666-88-9
RCSB PDB Ligand	AZ5
PubChem SID	488199394

化学和物理性质

溶解性	DMSO ≥68mg/mL Water <1.2mg/mL Ethanol ≥4.7mg/mL
密度	1.5
折光率	1.7
沸点	~575.2 °C at 760 mmHg
熔点	213.39°C

安全和危险性（GHS）

象形图	Toxic Health Hazard
信号词	Danger
危险声明	H301: Toxic if swallowed H372: Causes damage to organs through prolonged or repeated exposure H361: Suspected of damaging fertility or the unborn child
预防措施声明	P280,P321,P405,P501,P264,P260,P270,P330,P203,P301+P316,P318,P319

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参考文献

1. Ioannidis S, Lamb ML, Wang T, Almeida L, Block MH, Davies AM, Peng B, Su M, Zhang HJ, Hoffmann E et al.. (2011) Discovery of 5-chloro-N2-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine (AZD1480) as a novel inhibitor of the Jak/Stat pathway.. J Med Chem, 54 (1): (262-76). [PMID:21138246]