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AZD1480是一種新型,ATP競爭性的JAK2抑制劑,無細胞試驗中IC50為0.26 nM,選擇性作用于JAK3和Tyk2,對JAK1的作用較弱。Phase 1。
AZD1480 Chemical Structure
CAS: 935666-88-9
細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
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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 | ||
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產(chǎn)品描述 | AZD1480是一種新型,ATP競爭性的JAK2抑制劑,無細胞試驗中IC50為0.26 nM,選擇性作用于JAK3和Tyk2,對JAK1的作用較弱。Phase 1。 | ||
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特性 | AZD1480為治療多發(fā)性骨髓瘤的潛在新型治療劑。 | ||
靶點 |
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體外研究(In Vitro) | ||||
體外研究活性 | 5μM AZD1480誘導(dǎo)細胞周期停在G2/M期,且通過抑制Aurora激酶而誘導(dǎo)細胞死亡。[1]AZD1480是JAK2的有效抑制劑,作用于人類多發(fā)性骨髓瘤細胞,可以抑制生長,存活,F(xiàn)GFR3 和 STAT3信號,及下游靶點,包括 Cyclin D2。在低微摩爾濃度時,AZD1480抑制細胞增殖和誘導(dǎo)骨髓瘤細胞系凋亡。[2]AZD1480 作用于人和鼠神經(jīng)膠質(zhì)瘤細胞,有效抑制組成型和誘導(dǎo)型JAK1, JAK2, 及STAT-3的磷酸化作用 ,結(jié)果導(dǎo)致細胞增殖降低,且誘導(dǎo)凋亡。[3]AZD1480是有效的ATP競爭性的JAK1/2激酶小分子抑制劑,可抑制STAT3磷酸化和腫瘤生長,這種抑制存在STAT3依賴性。AZD1480通過影響腫瘤的微環(huán)境而抑制腫瘤血管生成和局部轉(zhuǎn)移。[4] | |||
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激酶實驗 | 激酶實驗 | |||
在有buffer(包括50 mM HEPES pH 為7.3, 1 mM DTT, 0.01% Tween-20, 50 μg/ml BSA,及10 mM MgCl2)的條件下,使用重組Jak1, Jak2, 或Jak3進行AZD1480抑制效果研究。在昆蟲細胞中,Jak3酶表達為氮端GST融合蛋白,且通過谷胱甘肽親和及尺寸排除色譜來純化Jak3酶。加入AZD1480 (10點劑量反應(yīng), 重復(fù)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 Km (Jak1: 55 μM, Jak2: 15 μM, Jak3: 3 μM),ATP濃度為5 mM,進行酶實驗。分離磷酸化和未磷酸化的肽段,使用Caliper LC3000系統(tǒng)計算抑制百分率。 | ||||
細胞實驗 | 細胞系 | Renca或786-O細胞,鼠內(nèi)皮細胞和脾CD11b+/c?骨髓細胞, HUVECs | ||
濃度 | 1 μM | |||
孵育時間 | 48或24小時 | |||
方法 | Renca或786-O細胞懸浮在含5%FBS的DMEM培養(yǎng)基中,按每孔5×103個細胞接種在96孔板上,使細胞粘附,實驗組用AZD1480,對照組用DMSO,處理48小時。通過MTS實驗測定細胞活力。使用Mikrotek Laborsysteme在490nm處測定吸光值。鼠內(nèi)皮細胞和脾CD11b+/c? 骨髓細胞從攜帶腫瘤的鼠中富集得到,培養(yǎng)在含5% FBS的RPMI-1640培養(yǎng)基上。HUVECs 培養(yǎng)在膠原1包被的含完全培養(yǎng)基的板上。用DMSO和不同劑量AZD1480處理所有細胞,持續(xù)24小時。手動計算細胞數(shù)而測定細胞活力。所有實驗重復(fù)三次。 | |||
實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | 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 |
體內(nèi)研究(In Vivo) | ||
體內(nèi)研究活性 | AZD1480作用于人類實體瘤模型和多發(fā)性骨髓瘤模型,抑制 STAT3磷酸化。[1]在體內(nèi), AZD1480抑制皮下移植瘤的生長,且通過抑制STAT3活性提高攜帶顱內(nèi)惡性膠質(zhì)瘤(GBM)的鼠壽命,說明AZD1480抑制JAK/STAT3通路的藥理學(xué)可以用于研究治療攜帶顱內(nèi)惡性膠質(zhì)瘤的患者。[3]AZD1480抑制骨髓細胞的肺浸潤和肺轉(zhuǎn)移瘤。AZD1480作用于人類移植瘤模型降低血管生成和代謝。[4]AZD1480抑制含有STAT活性的人類實體瘤的生長。[5] | |
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動物實驗 | Animal Models | 雌性BALB/c和無胸腺鼠(NCR? nu/nu) (7-8周大) |
Dosages | 每天一次,劑量為50 mg/kg;或者每天兩次,劑量為30 mg/kg | |
Administration | 口服飼喂 |
NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
---|---|---|---|---|---|
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 |
分子量 | 348.77 | 分子式 | C14H14ClFN8 |
CAS號 | 935666-88-9 | SDF | Download AZD1480 SDF |
Smiles | CC1=CC(=NN1)NC2=NC(=NC=C2Cl)NC(C)C3=NC=C(C=N3)F | ||
儲存條件(自收到貨起) | |||
體外溶解度 |
DMSO : 70 mg/mL ( (200.7 mM) ;DMSO吸濕會降低化合物溶解度,請使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計算器 |
體內(nèi)溶解度 現(xiàn)配現(xiàn)用,請按從左到右的順序依次添加,澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 |
動物體內(nèi)配方計算器(澄清溶液)
第一步:請輸入基本實驗信息(考慮到實驗過程中的損耗,建議多配一只動物的藥量)
第二步:請輸入動物體內(nèi)配方組成(配方適用于不溶于水的藥物;不同批次藥物配方比例不同,請聯(lián)系Selleck為您提供正確的澄清溶液配方)
計算結(jié)果:
工作液濃度: mg/ml;
DMSO母液配制方法: mg 藥物溶于μL DMSO溶液(母液濃度mg/mL,注:如該濃度超過該批次藥物DMSO溶解度,請先聯(lián)系Selleck);
體內(nèi)配方配制方法:取μL DMSO母液,加入μL PEG300,混勻澄清后加入μL Tween 80,混勻澄清后加入μL ddH2O,混勻澄清。
體內(nèi)配方配制方法:取μL DMSO母液,加入μL Corn oil,混勻澄清。
注意:1. 首先保證母液是澄清的;
2.一定要按照順序依次將溶劑加入,進行下一步操作之前必須保證上一步操作得到的是澄清的溶液,可采用渦旋、超聲或水浴加熱等物理方法助溶。
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