AZD1480

目录号：S2162 Purity: 99.16%

AZD1480是一种新型，ATP竞争性的JAK2抑制剂，无细胞试验中IC50为0.26 nM，选择性作用于JAK3和Tyk2，对JAK1的作用较弱。Phase 1。

AZD1480 Chemical Structure

CAS: 935666-88-9

规格	价格	库存
10mM (1mL in DMSO)	1071.19	现货
5mg	819.48	现货
50mg	4671.71	现货
200mg	12858.3	现货
1g	43161.3	现货
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产品质控

批次：纯度： 99.16%

99.16

AZD1480相关产品

相关靶点	JAK1 JAK2 JAK3 Tyk2	点击展开
相关产品	WP1066 Momelotinib (CYT387) Filgotinib (GLPG0634) AT9283 Gandotinib (LY2784544) TG101209 Cerdulatinib (PRT062070) hydrochloride Pacritinib NVP-BSK805 2HCl WHI-P154 FLLL32 Decernotinib (VX-509) CEP-33779 AZ 960 Cerdulatinib (PRT062070) ZM 39923 HCl XL019 BMS-911543 Curcumol Solcitinib Oclacitinib maleate Pyridone 6 Creatine Ritlecitinib (PF-06651600) Deucravacitinib (BMS-986165) Itacitinib (INCB39110) Peficitinib BD750 WHI-P97 JANEX-1 Brevilin A 1,2,3,4,5,6-Hexabromocyclohexane Brepocitinib (PF-06700841) FM-381 SAR-20347 Selective JAK3 inhibitor 1	点击展开
相关化合物库	激酶抑制剂库 FDA药物库天然产物库酪氨酸激酶抑制剂分子库 JAK-STAT信号通路库	点击展开

细胞实验数据示例

细胞系	实验类型	给药浓度	孵育时间	活性描述	文献信息
NCI-H82	Apoptosis Assay	0.3/1/3 μM	48 h	increases the level of cleaved-Caspase 3	24158701
GLC4	Apoptosis Assay	0.3/1/3 μM	48 h	increases the level of cleaved-Caspase 3	24158701
NCI-N592	Apoptosis Assay	0.3/1/3 μM	48 h	increases the level of cleaved-Caspase 3	24158701
NCI-H82	Function Assay	0.3/1/3 μM	24 h	induces G2/M cell cycle arrest	24158701
GLC4	Function Assay	0.3/1/3 μM	24 h	induces G2/M cell cycle arrest	24158701
NCI-N592	Function Assay	0.3/1/3 μM	24 h	induces G2/M cell cycle arrest	24158701
CWR22Rv1	Function Assay	800 nM	72 h	suppresses IL-6-induced migratory	24577942
DU145	Function Assay	800 nM	72 h	suppresses IL-6-induced migratory	24577942
DU145	Function Assay	0-200 nM	1 h	suppresses IL-6-activated Stat3 and ERK1/2 signaling	24577942
MO4	Function Assay	0.5/1/5 μM	6 h	inhibits P-STAT3 expression	25149535
OVCAR-8	Apoptosis Assay	0.5/1/5 μM	48 h	induces significant apoptosis at high concerntration	25646015
OVCAR-5	Apoptosis Assay	0.5/1/5 μM	48 h	induces significant apoptosis at high concerntration	25646015
OVCAR-8	Cell Viability Assay	0.05-10 μM	72 h	reduces cell viability at the concerntration of 5 μM	25646015
OVCAR-5	Cell Viability Assay	0.05-10 μM	72 h	reduces cell viability at the concerntration of 5 μM	25646015
A1847	Cell Viability Assay	0.05-10 μM	72 h	reduces cell viability at the concerntration of 5 μM	25646015
MOVCAR-5009	Function Assay	0.05-10 μM	24 h	reduces phosphorylated STAT3 levels	25646015
MOVCAR-5447	Function Assay	0.05-10 μM	24 h	reduces phosphorylated STAT3 levels	25646015
OVCAR-8	Function Assay	0.05-10 μM	24 h	reduces phosphorylated STAT3 levels	25646015
OVCAR-5	Function Assay	0.05-10 μM	24 h	reduces phosphorylated STAT3 levels	25646015
A1847	Function Assay	0.05-10 μM	24 h	reduces phosphorylated STAT3 levels	25646015
UM-22A	Function Assay	0.0005-1.6 μM	24 h	abrogates IL-6–induced up-regulation of pSTAT3Tyr705 in a dose-dependent manner	25810010
HH5	Function Assay	0.0005-3.8 μM	24 h	abrogates IL-6–induced up-regulation of pSTAT3Tyr705 in a dose-dependent manner	25810010
Cal33	Function Assay	0.0005-3.8 μM	24 h	abrogates IL-6–induced up-regulation of pSTAT3Tyr705 in a dose-dependent manner	25810010
UMSCC-1	Function Assay	0.0005-1.6 μM	24 h	abrogates IL-6–induced up-regulation of pSTAT3Tyr705 in a dose-dependent manner	25810010
LoVo	Function Assay	5 μM	48 h	blocks JAK2/STAT3 signaling	25954974
SW620	Function Assay	5 μM	48 h	blocks JAK2/STAT3 signaling	25954974
KCNR	Apoptosis Assay	0.5/1.0/2.5 μM	24 h	induces an increase in caspase 3/7 activity	23531921
SY5Y	Apoptosis Assay	0.5/1.0/2.5 μM	24 h	induces an increase in caspase 3/7 activity	23531921
Rh18	Apoptosis Assay	0.5/1.0/2.5 μM	24 h	induces an increase in caspase 3/7 activity	23531921
TC32	Apoptosis Assay	0.5/1.0/2.5 μM	24 h	induces an increase in caspase 3/7 activity	23531921
KCNR	Function Assay	0.5/1.0/2.5/5 μM	24 h	inhibits both endogenous constitutive and IL-6-induced STAT3 activation	23531921
SY5Y	Function Assay	0.5/1.0/2.5/5 μM	24 h	inhibits both endogenous constitutive and IL-6-induced STAT3 activation	23531921
Rh18	Function Assay	0.5/1.0/2.5/5 μM	24 h	inhibits both endogenous constitutive and IL-6-induced STAT3 activation	23531921
TC32	Function Assay	0.5/1.0/2.5/5 μM	24 h	inhibits both endogenous constitutive and IL-6-induced STAT3 activation	23531921
TPC-1	Growth Inhibition Assay	1 µM	0-4 d	inhibits cell growth after 2 d treatment	23056499
MZ-CRC1	Growth Inhibition Assay	1 µM	0-5 d	inhibits cell growth after 1 d treatment	23056499
TT	Growth Inhibition Assay	1 µM	0-4 d	inhibits cell growth after 1 d treatment	23056499
TPC-1	Function Assay	1 µM	72 h	induces G1 blockage	23056499
MZ-CRC1	Function Assay	1 µM	72 h	induces G1 blockage	23056499
TT	Function Assay	1 µM	72 h	induces G1 blockage	23056499
MZ-CRC1	Apoptosis Assay	1 µM	48 h	induces apoptosis	23056499
TT	Apoptosis Assay	1 µM	48 h	induces apoptosis	23056499
HD-LM2	Function Assay	0.1/0.5/1/5 μM	72 h	inhibits STAT3, STAT5 and STAT6 phosphorylation	22829094
L-428	Function Assay	0.1/0.5/1/5 μM	72 h	inhibits STAT3, STAT5 and STAT6 phosphorylation	22829094
KM-H2	Function Assay	0.1/0.5/1/5 μM	72 h	inhibits STAT3, STAT5 and STAT6 phosphorylation	22829094
L-540	Function Assay	0.1/0.5/1/5 μM	72 h	inhibits STAT3, STAT5 and STAT6 phosphorylation	22829094
HD-LM2	Apoptosis Assay	1/5 μM	72 h	induces apoptosis	22829094
L-428	Apoptosis Assay	1/5 μM	72 h	induces apoptosis	22829094
KM-H2	Apoptosis Assay	1/5 μM	72 h	induces apoptosis	22829094
L-540	Apoptosis Assay	1/5 μM	72 h	induces apoptosis	22829094
U251-MG	Function Assay	1 µM	0-16 h	inhibits constitutive STAT-3 and JAK2 activation	22027691
U87-MG	Function Assay	1 µM	0-16 h	inhibits constitutive STAT-3 and JAK2 activation	22027691
4C8	Function Assay	1 µM	0-16 h	inhibits constitutive STAT-3 and JAK2 activation	22027691
U251-MG	Growth Inhibition Assay	1/10 µM	24/48/72 h	inhibits cell proliferation at a concentration of 10 µM	22027691
U87-MG	Growth Inhibition Assay	1/10 µM	24/48/72 h	inhibits cell proliferation at a concentration of 10 µM	22027691
4C8	Growth Inhibition Assay	1/10 µM	24/48/72 h	inhibits cell proliferation at a concentration of 10 µM	22027691
U266	Apoptosis Assay	0.5-2 μM	48/72 h	induces apoptosis dose dependently	21164517
Kms.11	Apoptosis Assay	0.5-2 μM	48/72 h	induces apoptosis dose dependently	21164517
8226	Apoptosis Assay	0.5-2 μM	48/72 h	induces apoptosis dose dependently	21164517
SW620	Cell cycle assay	3.3 uM	24 hrs	Cell cycle arrest in human SW620 cells assessed as accumulation at G2/M phase at 3.3 uM after 24 hrs by flow cytometry	21138246
HEL	Function assay	0.3 uM	5 mins	Inhibition of Stat5 phosphorylation in human HEL cells at 0.3 uM after 5 mins by Western blotting	21138246
HEL	Function assay	0.3 uM	30 to 60 mins	Inhibition of Stat5 phosphorylation in human HEL cells at 0.3 uM after 30 to 60 mins by Western blotting	21138246
BA/F3	Antitumor assay	30 mg/kg	12 hrs	Antitumor activity against mouse BA/F3 cells expressing Tel-JAK2 xenografted in NCr mouse assessed as reduction of phosphorylated Stat5 level in spleen at 30 mg/kg, po after 12 hrs by Western blotting	21138246
HEL	Function assay	0.3 uM	5 mins	Inhibition of Stat3 phosphorylation in human HEL cells at 0.3 uM after 5 mins by Western blotting	21138246
HEL	Function assay	0.3 uM	30 to 60 mins	Inhibition of Stat3 phosphorylation in human HEL cells at 0.3 uM after 30 to 60 mins by Western blotting	21138246
Hs578T	Function assay	1 uM	24 hrs	Inhibition of STAT3C-mediated transcription in human Hs578T cells at 1 uM after 24 hrs by luciferase reporter gene assay	24978112
NCI-H1975	Function assay	0.003 to 3 uM	2 hrs	Inhibition of JAK1 in human NCI-H1975 cells assessed as reduction in STAT3 phosphorylation at 0.003 to 3 uM after 2 hrs by Western blot analysis	26614408
PALJDL	Cell Viability Assay		72 h	IC50=2.4 μM	25504635
AKRSL	Cell Viability Assay		72 h	IC50＞10 μM	25504635
PCI-15B	Growth Inhibition Assay		72 h	EC50=0.99 ± 1.74 μM	25810010
PCI-52	Growth Inhibition Assay		72 h	EC50=1.00 ± 0.09 μM	25810010
OSC19	Growth Inhibition Assay		72 h	EC50=1.26 ± 0.20 μM	25810010
UM-22A	Growth Inhibition Assay		72 h	EC50=1.32 ± 0.39 μM	25810010
UM SCC-1	Growth Inhibition Assay		72 h	EC50=1.67 ± 0.42 μM	25810010
686LN	Growth Inhibition Assay		72 h	EC50=2.05 ± 1.33 μM	25810010
UM-22B	Growth Inhibition Assay		72 h	EC50=2.66 ± 0.24 μM	25810010
Cal33	Growth Inhibition Assay		72 h	EC50=3.37 ± 0.75 μM	25810010
HN5	Growth Inhibition Assay		72 h	EC50=3.81 ± 1.99 μM	25810010
HD-LM2	Growth Inhibition Assay		72 h	IC50=7.844 μM	22829094
L-428	Growth Inhibition Assay		72 h	IC50=7.947 μM	22829094
KM-H2	Growth Inhibition Assay		72 h	IC50=1.308 μM	22829094
L-540	Growth Inhibition Assay		72 h	IC50=8.216 μM	22829094
SET2	Growth inhibition assay		48 hrs	Growth inhibition of human SET2 cells expressing Jak2 V617F mutant after 48 hrs by MTS assay, GI50 = 0.016 μM.	21138246
SET2	Function assay		1 hr	Inhibition of Stat3 phosphorylation in human SET2 cells after 1 hr by Western blotting, IC50 = 0.023 μM.	21138246
SET2	Function assay		1 hr	Inhibition of Stat5 phosphorylation in human SET2 cells after 1 hr by Western blotting, IC50 = 0.025 μM.	21138246
HEL	Function assay		1 hr	Inhibition of Stat5 phosphorylation in human HEL cells after 1 hr by Western blotting, IC50 = 0.041 μM.	21138246
UKE1	Growth inhibition assay		48 hrs	Growth inhibition of human UKE1 cells expressing Jak2 V617F mutant after 48 hrs by MTS assay, GI50 = 0.054 μM.	21138246
BA/F3	Growth inhibition assay		48 hrs	Growth inhibition of mouse BA/F3 cells expressing Tel-JAK2 kinase after 48 hrs by MTS assay, GI50 = 0.06 μM.	21138246
HEL	Function assay		1 hr	Inhibition of Stat3 phosphorylation in human HEL cells after 1 hr by Western blotting, IC50 = 0.08 μM.	21138246
HEL	Growth inhibition assay		48 hrs	Growth inhibition of human HEL cells expressing Jak2 V617F mutant after 48 hrs by MTS assay, GI50 = 0.39 μM.	21138246
BA/F3	Growth inhibition assay		48 hrs	Growth inhibition of mouse BA/F3 cells expressing Tel-JAK1 kinase after 48 hrs by MTS assay, GI50 = 0.7 μM.	21138246
BA/F3	Growth inhibition assay		48 hrs	Growth inhibition of mouse BA/F3 cells expressing Tel-Tyk2 kinase after 48 hrs by MTS assay, GI50 = 2 μM.	21138246
BA/F3	Growth inhibition assay		48 hrs	Growth inhibition of mouse BA/F3 cells expressing Tel-JAK3 kinase after 48 hrs by MTS assay, GI50 = 2.1 μM.	21138246
UKE1	Function assay		1 hr	Inhibition of Stat5 phosphorylation in human UKE1 cells after 1 hr by Western blotting	21138246
HEL 92.1.7	Function assay		2 hrs	Inhibition of JAK2 in human HEL 92.1.7 cells assessed as reduction in STAT5 phosphorylation after 2 hrs by Western blot analysis	26614408
IMR32	Growth Inhibition Assay			IC50=0.66 μM	23531921
NGP	Growth Inhibition Assay			IC50=0.56 μM	23531921
AS	Growth Inhibition Assay			IC50=1.53 μM	23531921
BE2	Growth Inhibition Assay			IC50=0.71 μM	23531921
SY5Y	Growth Inhibition Assay			IC50=0.36 μM	23531921
KCNR	Growth Inhibition Assay			IC50=0.46 μM	23531921
HEK293	Growth Inhibition Assay			IC50=8.67 μM	23531921
ARPE19	Growth Inhibition Assay			IC50=24.38 μM	23531921
RC165N	Apoptosis Assay			IC50=2.083 μM	23942095
DU145	Apoptosis Assay			IC50=3.517 μM	23942095
PC-3	Apoptosis Assay			IC50=1.755 μM	23942095
CWR22Pc	Apoptosis Assay			IC50=0.438 μM	23942095
CWR22Rv1	Apoptosis Assay			IC50=0.482 μM	23942095
DMS114	Growth Inhibition Assay			IC50=0.73 μM	24158701
H1173	Growth Inhibition Assay			IC50=2.39 μM	24158701
H526	Growth Inhibition Assay			IC50=3.08 μM	24158701
GLC4	Growth Inhibition Assay			IC50=1.79 μM	24158701
H82	Growth Inhibition Assay			IC50=1.37 μM	24158701
N592	Growth Inhibition Assay			IC50=0.84 μM	24158701
LAN5	Growth Inhibition Assay			IC50=1.04 μM	23531921
RH18	Growth Inhibition Assay			IC50=1.42 μM	23531921
RH30	Growth Inhibition Assay			IC50=1.25 μM	23531921
RH17	Growth Inhibition Assay			IC50=2.51 μM	23531921
RH28	Growth Inhibition Assay			IC50=4.28 μM	23531921
RH36	Growth Inhibition Assay			IC50=5.37 μM	23531921
RH41	Growth Inhibition Assay			IC50=0.48 μM	23531921
RD	Growth Inhibition Assay			IC50=4.32 μM	23531921
TC32	Growth Inhibition Assay			IC50=3.85 μM	23531921
TC71	Growth Inhibition Assay			IC50=4.33 μM	23531921
Ba/F3	Function assay			Inhibition of Stat5 phosphorylation in mouse Ba/F3 cells expressing TEL-Jak2, IC50 = 0.046 μM.	21138246
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
点击查看更多细胞系数据

生物活性

产品描述

AZD1480是一种新型，ATP竞争性的JAK2抑制剂，无细胞试验中IC50为0.26 nM，选择性作用于JAK3和Tyk2，对JAK1的作用较弱。Phase 1。

特性

AZD1480为治疗多发性骨髓瘤的潜在新型治疗剂。

靶点

JAK2 ^[1]
(Cell-free assay)

0.26 nM

体外研究(In Vitro)
体外研究活性	5μM AZD1480诱导细胞周期停在G2/M期，且通过抑制Aurora激酶而诱导细胞死亡。^[1]AZD1480是JAK2的有效抑制剂，作用于人类多发性骨髓瘤细胞，可以抑制生长，存活，FGFR3 和 STAT3信号，及下游靶点，包括 Cyclin D2。在低微摩尔浓度时，AZD1480抑制细胞增殖和诱导骨髓瘤细胞系凋亡。^[2]AZD1480 作用于人和鼠神经胶质瘤细胞，有效抑制组成型和诱导型JAK1, JAK2, 及STAT-3的磷酸化作用，结果导致细胞增殖降低，且诱导凋亡。^[3]AZD1480是有效的ATP竞争性的JAK1/2激酶小分子抑制剂，可抑制STAT3磷酸化和肿瘤生长，这种抑制存在STAT3依赖性。AZD1480通过影响肿瘤的微环境而抑制肿瘤血管生成和局部转移。^[4]
激酶实验	激酶实验
激酶实验	在有buffer(包括50 mM HEPES pH 为7.3, 1 mM DTT, 0.01% Tween-20, 50 µg/ml BSA,及10 mM MgCl₂)的条件下，使用重组Jak1, Jak2, 或Jak3进行AZD1480抑制效果研究。在昆虫细胞中，Jak3酶表达为氮端GST融合蛋白，且通过谷胱甘肽亲和及尺寸排除色谱来纯化Jak3酶。加入AZD1480 (10点剂量反应, 重复三次, 8.3 µM 到0.3 nM )，使用1.5 µM 肽底物(Jak1:FITC-C6-KKHTDDGYMPMSPGVA-NH2, Jak2和Jak3: FAM-SRCtide)，及各自ATP K_m (Jak1: 55 µM, Jak2: 15 µM, Jak3: 3 µM)，ATP浓度为5 mM，进行酶实验。分离磷酸化和未磷酸化的肽段，使用Caliper LC3000系统计算抑制百分率。
细胞实验	细胞系	Renca或786-O细胞，鼠内皮细胞和脾CD11b+/c−骨髓细胞, HUVECs
	浓度	1 μM
	孵育时间	48或24小时
	方法	Renca或786-O细胞悬浮在含5%FBS的DMEM培养基中,按每孔5×10³个细胞接种在96孔板上，使细胞粘附，实验组用AZD1480，对照组用DMSO，处理48小时。通过MTS实验测定细胞活力。使用Mikrotek Laborsysteme在490nm处测定吸光值。鼠内皮细胞和脾CD11b+/c− 骨髓细胞从携带肿瘤的鼠中富集得到，培养在含5% FBS的RPMI-1640培养基上。HUVECs 培养在胶原1包被的含完全培养基的板上。用DMSO和不同剂量AZD1480处理所有细胞，持续24小时。手动计算细胞数而测定细胞活力。所有实验重复三次。
实验图片	检测方法	检测指标	实验图片	PMID
	Western blot	p-STAT3 / STAT3 / p-JAK2 / JAK2 p-STAT1 / STAT1 / p-STAT5 / STAT5 / p-STAT6 / STAT6 p-ERK / ERK / p-p38 / p38 / SOCS3 / p-SHP2 / SHP2		22027691
	Immunofluorescence	pSTAT5		30140255
	Growth inhibition assay	Cell proliferation Cell viability		22027691

体内研究(In Vivo)
体内研究活性	AZD1480作用于人类实体瘤模型和多发性骨髓瘤模型，抑制 STAT3磷酸化。^[1]在体内, AZD1480抑制皮下移植瘤的生长，且通过抑制STAT3活性提高携带颅内恶性胶质瘤(GBM)的鼠寿命，说明AZD1480抑制JAK/STAT3通路的药理学可以用于研究治疗携带颅内恶性胶质瘤的患者。^[3]AZD1480抑制骨髓细胞的肺浸润和肺转移瘤。AZD1480作用于人类移植瘤模型降低血管生成和代谢。^[4]AZD1480抑制含有STAT活性的人类实体瘤的生长。^[5]
动物实验	Animal Models	雌性BALB/c和无胸腺鼠(NCR− nu/nu) (7-8周大)
	Dosages	每天一次，剂量为50 mg/kg；或者每天两次，剂量为30 mg/kg
	Administration	口服饲喂

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT01219543	Terminated	Solid Tumour\|Advanced Solid Malignancies\|Child-Pugh A to B7 Advanced Hepatocellular Carcinoma\|EGFR and/or ROS Mutant NSCLC\|Lung Metastasis Carcinoma\|Gastric Cancer	AstraZeneca	November 2010	Phase 1
NCT01112397	Terminated	Solid Malignancies	AstraZeneca	April 2010	Phase 1

参考文献
[1] E Derenzini, et al. Blood Cancer J, 2011, 1(12), e46. [2] Scuto A, et al. Leukemia, 2011, 25(3), 538-50. [3] McFarland BC,et al. Cancer Ther, 2011, 10(12), 2384-93. [4] Xin H, et al. Cancer Res, 2011, 71(21), 6601-10. [5] Hedvat M, et al. Cancer Cell, 2009, 16(6), 487-97. + 展开

参考文献

+ 展开

化学信息&溶解度

分子量	348.77	分子式	C₁₄H₁₄ClFN₈
CAS号	935666-88-9	SDF	Download AZD1480 SDF
Smiles	CC1=CC(=NN1)NC2=NC(=NC=C2Cl)NC(C)C3=NC=C(C=N3)F
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

DMSO : 70 mg/mL ( (200.7 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 70 mg/mL ( (200.7 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 70 mg/mL ( (200.7 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 70 mg/mL ( (200.7 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 23 mg/mL ( (65.94 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解配方批次：现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂				动物体内配方计算器
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	5.000mg/ml (14.34mM)	以 1 mL 工作液为例,取50μL100mg/ml的澄清DMSO储备液加到400μLPEG300中,混合均匀使其澄清;向上述体系中加入50μLTween80,混合均匀使其澄清;然后继续加入500μLddH2O定容至1mL。工作液请现配现用!
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	5.000mg/ml (14.34mM)	以 1 mL 工作液为例，取50μL100mg/ml的澄清DMSO储备液加到400μL PEG300中，混合均匀使其澄清；向上述体系中加入50μLTween80，混合均匀使其澄清；然后继续加入500μL ddH2O定容至 1 mL。工作液请现配现用！
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

* 必填项

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

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