연구용
제품 번호: S2162
화학 구조
| 세포주 | 분석 유형 | 농도 | 배양 시간 | 제형 | 활성 설명 | PMID |
|---|---|---|---|---|---|---|
| SW620 | Function Assay | 5 μM | 48 h | DMSO | blocks JAK2/STAT3 signaling | 25954974 |
| LoVo | Function Assay | 5 μM | 48 h | DMSO | blocks JAK2/STAT3 signaling | 25954974 |
| HN5 | Growth Inhibition Assay | 72 h | EC50=3.81 ± 1.99 μM | 25810010 | ||
| Cal33 | Growth Inhibition Assay | 72 h | EC50=3.37 ± 0.75 μM | 25810010 | ||
| UM-22B | Growth Inhibition Assay | 72 h | EC50=2.66 ± 0.24 μM | 25810010 | ||
| 686LN | Growth Inhibition Assay | 72 h | EC50=2.05 ± 1.33 μM | 25810010 | ||
| UM SCC-1 | Growth Inhibition Assay | 72 h | EC50=1.67 ± 0.42 μM | 25810010 | ||
| UM-22A | Growth Inhibition Assay | 72 h | EC50=1.32 ± 0.39 μM | 25810010 | ||
| OSC19 | Growth Inhibition Assay | 72 h | EC50=1.26 ± 0.20 μM | 25810010 | ||
| PCI-52 | Growth Inhibition Assay | 72 h | EC50=1.00 ± 0.09 μM | 25810010 | ||
| PCI-15B | Growth Inhibition Assay | 72 h | EC50=0.99 ± 1.74 μM | 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 | |
| Cal33 | Function Assay | 0.0005-3.8 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 | |
| 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 | |
| A1847 | Function Assay | 0.05-10 μM | 24 h | DMSO | reduces phosphorylated STAT3 levels | 25646015 |
| OVCAR-5 | Function Assay | 0.05-10 μM | 24 h | DMSO | reduces phosphorylated STAT3 levels | 25646015 |
| OVCAR-8 | Function Assay | 0.05-10 μM | 24 h | DMSO | reduces phosphorylated STAT3 levels | 25646015 |
| MOVCAR-5447 | Function Assay | 0.05-10 μM | 24 h | DMSO | reduces phosphorylated STAT3 levels | 25646015 |
| MOVCAR-5009 | Function Assay | 0.05-10 μM | 24 h | DMSO | reduces phosphorylated STAT3 levels | 25646015 |
| A1847 | Cell Viability Assay | 0.05-10 μM | 72 h | DMSO | reduces cell viability at the concerntration of 5 μM | 25646015 |
| OVCAR-5 | Cell Viability Assay | 0.05-10 μM | 72 h | DMSO | reduces cell viability at the concerntration of 5 μM | 25646015 |
| OVCAR-8 | Cell Viability Assay | 0.05-10 μM | 72 h | DMSO | reduces cell viability at the concerntration of 5 μM | 25646015 |
| OVCAR-5 | Apoptosis Assay | 0.5/1/5 μM | 48 h | DMSO | induces significant apoptosis at high concerntration | 25646015 |
| OVCAR-8 | Apoptosis Assay | 0.5/1/5 μM | 48 h | DMSO | induces significant apoptosis at high concerntration | 25646015 |
| AKRSL | Cell Viability Assay | 72 h | IC50>10 μM | 25504635 | ||
| PALJDL | Cell Viability Assay | 72 h | IC50=2.4 μM | 25504635 | ||
| MO4 | Function Assay | 0.5/1/5 μM | 6 h | inhibits P-STAT3 expression | 25149535 | |
| DU145 | Function Assay | 0-200 nM | 1 h | suppresses IL-6-activated Stat3 and ERK1/2 signaling | 24577942 | |
| DU145 | Function Assay | 800 nM | 72 h | suppresses IL-6-induced migratory | 24577942 | |
| CWR22Rv1 | Function Assay | 800 nM | 72 h | suppresses IL-6-induced migratory | 24577942 | |
| N592 | Growth Inhibition Assay | IC50=0.84 μM | 24158701 | |||
| H82 | Growth Inhibition Assay | IC50=1.37 μM | 24158701 | |||
| GLC4 | Growth Inhibition Assay | IC50=1.79 μM | 24158701 | |||
| H526 | Growth Inhibition Assay | IC50=3.08 μM | 24158701 | |||
| H1173 | Growth Inhibition Assay | IC50=2.39 μM | 24158701 | |||
| DMS114 | Growth Inhibition Assay | IC50=0.73 μM | 24158701 | |||
| NCI-N592 | 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-H82 | Function Assay | 0.3/1/3 μM | 24 h | induces G2/M cell cycle arrest | 24158701 | |
| NCI-N592 | 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-H82 | Apoptosis Assay | 0.3/1/3 μM | 48 h | increases the level of cleaved-Caspase 3 | 24158701 | |
| CWR22Rv1 | Apoptosis Assay | IC50=0.482 μM | 23942095 | |||
| CWR22Pc | Apoptosis Assay | IC50=0.438 μM | 23942095 | |||
| PC-3 | Apoptosis Assay | IC50=1.755 μM | 23942095 | |||
| DU145 | Apoptosis Assay | IC50=3.517 μM | 23942095 | |||
| RC165N | Apoptosis Assay | IC50=2.083 μM | 23942095 | |||
| ARPE19 | Growth Inhibition Assay | DMSO | IC50=24.38 μM | 23531921 | ||
| HEK293 | Growth Inhibition Assay | DMSO | IC50=8.67 μM | 23531921 | ||
| KCNR | Growth Inhibition Assay | DMSO | IC50=0.46 μM | 23531921 | ||
| SY5Y | Growth Inhibition Assay | DMSO | IC50=0.36 μM | 23531921 | ||
| BE2 | Growth Inhibition Assay | DMSO | IC50=0.71 μM | 23531921 | ||
| AS | Growth Inhibition Assay | DMSO | IC50=1.53 μM | 23531921 | ||
| NGP | Growth Inhibition Assay | DMSO | IC50=0.56 μM | 23531921 | ||
| IMR32 | Growth Inhibition Assay | DMSO | IC50=0.66 μM | 23531921 | ||
| LAN5 | Growth Inhibition Assay | DMSO | IC50=1.04 μM | 23531921 | ||
| RH18 | Growth Inhibition Assay | DMSO | IC50=1.42 μM | 23531921 | ||
| RH30 | Growth Inhibition Assay | DMSO | IC50=1.25 μM | 23531921 | ||
| RH17 | Growth Inhibition Assay | DMSO | IC50=2.51 μM | 23531921 | ||
| RH28 | Growth Inhibition Assay | DMSO | IC50=4.28 μM | 23531921 | ||
| RH36 | Growth Inhibition Assay | DMSO | IC50=5.37 μM | 23531921 | ||
| RH41 | Growth Inhibition Assay | DMSO | IC50=0.48 μM | 23531921 | ||
| RD | Growth Inhibition Assay | DMSO | IC50=4.32 μM | 23531921 | ||
| TC32 | Growth Inhibition Assay | DMSO | IC50=3.85 μM | 23531921 | ||
| TC71 | Growth Inhibition Assay | DMSO | IC50=4.33 μM | 23531921 | ||
| KCNR | Apoptosis Assay | 0.5/1.0/2.5 μM | 24 h | DMSO | induces an increase in caspase 3/7 activity | 23531921 |
| SY5Y | Apoptosis Assay | 0.5/1.0/2.5 μM | 24 h | DMSO | induces an increase in caspase 3/7 activity | 23531921 |
| Rh18 | Apoptosis Assay | 0.5/1.0/2.5 μM | 24 h | DMSO | induces an increase in caspase 3/7 activity | 23531921 |
| TC32 | Apoptosis Assay | 0.5/1.0/2.5 μM | 24 h | DMSO | induces an increase in caspase 3/7 activity | 23531921 |
| KCNR | Function Assay | 0.5/1.0/2.5/5 μM | 24 h | DMSO | inhibits both endogenous constitutive and IL-6-induced STAT3 activation | 23531921 |
| SY5Y | Function Assay | 0.5/1.0/2.5/5 μM | 24 h | DMSO | inhibits both endogenous constitutive and IL-6-induced STAT3 activation | 23531921 |
| Rh18 | Function Assay | 0.5/1.0/2.5/5 μM | 24 h | DMSO | inhibits both endogenous constitutive and IL-6-induced STAT3 activation | 23531921 |
| TC32 | Function Assay | 0.5/1.0/2.5/5 μM | 24 h | DMSO | inhibits both endogenous constitutive and IL-6-induced STAT3 activation | 23531921 |
| TPC-1 | Growth Inhibition Assay | 1 µM | 0-4 d | DMSO | inhibits cell growth after 2 d treatment | 23056499 |
| MZ-CRC1 | Growth Inhibition Assay | 1 µM | 0-5 d | DMSO | inhibits cell growth after 1 d treatment | 23056499 |
| TT | Growth Inhibition Assay | 1 µM | 0-4 d | DMSO | inhibits cell growth after 1 d treatment | 23056499 |
| TPC-1 | Function Assay | 1 µM | 72 h | DMSO | induces G1 blockage | 23056499 |
| MZ-CRC1 | Function Assay | 1 µM | 72 h | DMSO | induces G1 blockage | 23056499 |
| TT | Function Assay | 1 µM | 72 h | DMSO | induces G1 blockage | 23056499 |
| MZ-CRC1 | Apoptosis Assay | 1 µM | 48 h | DMSO | induces apoptosis | 23056499 |
| TT | Apoptosis Assay | 1 µM | 48 h | DMSO | induces apoptosis | 23056499 |
| HD-LM2 | Growth Inhibition Assay | 72 h | DMSO | IC50=7.844 μM | 22829094 | |
| L-428 | Growth Inhibition Assay | 72 h | DMSO | IC50=7.947 μM | 22829094 | |
| KM-H2 | Growth Inhibition Assay | 72 h | DMSO | IC50=1.308 μM | 22829094 | |
| L-540 | Growth Inhibition Assay | 72 h | DMSO | IC50=8.216 μM | 22829094 | |
| HD-LM2 | Function Assay | 0.1/0.5/1/5 μM | 72 h | DMSO | inhibits STAT3, STAT5 and STAT6 phosphorylation | 22829094 |
| L-428 | Function Assay | 0.1/0.5/1/5 μM | 72 h | DMSO | inhibits STAT3, STAT5 and STAT6 phosphorylation | 22829094 |
| KM-H2 | Function Assay | 0.1/0.5/1/5 μM | 72 h | DMSO | inhibits STAT3, STAT5 and STAT6 phosphorylation | 22829094 |
| L-540 | Function Assay | 0.1/0.5/1/5 μM | 72 h | DMSO | inhibits STAT3, STAT5 and STAT6 phosphorylation | 22829094 |
| HD-LM2 | Apoptosis Assay | 1/5 μM | 72 h | DMSO | induces apoptosis | 22829094 |
| L-428 | Apoptosis Assay | 1/5 μM | 72 h | DMSO | induces apoptosis | 22829094 |
| KM-H2 | Apoptosis Assay | 1/5 μM | 72 h | DMSO | induces apoptosis | 22829094 |
| L-540 | Apoptosis Assay | 1/5 μM | 72 h | DMSO | 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 | |
| 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 | ||
| Ba/F3 | Function assay | Inhibition of Stat5 phosphorylation in mouse Ba/F3 cells expressing TEL-Jak2, IC50 = 0.046 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 | ||
| 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 | |
| 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 | ||
| 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 | |||
| 클릭하여 더 많은 세포주 실험 데이터 보기 | ||||||
| 분자량 | 348.77 | 화학식 | C14H14ClFN8 |
보관 (수령일로부터) | |
|---|---|---|---|---|---|
| CAS 번호 | 935666-88-9 | SDF 다운로드 | 원액 보관 |
|
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| 동의어 | N/A | Smiles | CC1=CC(=NN1)NC2=NC(=NC=C2Cl)NC(C)C3=NC=C(C=N3)F | ||
|
In vitro |
DMSO
: 70 mg/mL
(200.7 mM)
Water : Insoluble Ethanol : Insoluble |
|
In vivo |
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1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)
2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)
계산 결과:
작업 농도: mg/ml;
DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )
생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH2O, 혼합하고 투명하게 합니다.
생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.
참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.
| Targets/IC50/Ki |
JAK2
(Cell-free assay) 0.26 nM
|
|---|---|
| 시험관 내(In vitro) |
5μM AZD1480 induces G2/M arrest and cell death by inhibiting Aurora kinases. This compound 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, it blocks cell proliferation and induces apoptosis of myeloma cell lines. This chemical 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. It 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. This inhibitor inhibits tumor angiogenesis and metastasis in part by affecting the tumor microenvironment.
|
| 키나아제 분석 |
kinase assays
|
|
AZD1480의 저해 연구는 50 mM HEPES pH 7.3, 1 mM DTT, 0.01% Tween-20, 50 mM/ml BSA 및 10 mM MgCl2 완충 조건 하에서 재조합 Jak1, Jak2 또는 Jak3를 사용하여 수행된다. Jak3 효소는 곤충 세포에서 N-말단 GST 융합으로 발현되며 글루타치온 친화성 크로마토그래피 및 크기 배제 크로마토그래피를 통해 정제된다. 효소는 본 화합물 존재 하에(8.3 μM에서 0.3 nM까지 반로그 희석 단계로 3중 반복 수행하는 10포인트 용량 반응) 1.5 μM 펩타이드 기질(Jak1: FITC-C6-KKHTDDGYMPMSPGVA-NH2, Jak2 및 Jak3: FAM-SRCtide)을 사용하여 분석하며, 각 효소의 ATP Km(Jak1: 55 μM, Jak2: 15 μM, Jak3: 3 μM) 및 5 mM의 근사 생리학적 ATP 농도 조건 하에서 스크리닝된다. 인산화된 펩타이드와 비인산화된 펩타이드는 Caliper LC3000 시스템으로 분리 및 정량화되어 백분율 저해율을 계산한다.
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|
| 생체 내(In vivo) |
AZD1480 inhibits the STAT3 phosphorylation in an xenograft model of human solid tumors and multiple myeloma. In vivo, this compound 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 this chemical should be considered for study in the treatment of patients with GBM tumors. It blocks lung infiltration of myeloid cells and formation of pulmonary metastases in both mouse syngeneic experimental and spontaneous metastatic models. Furthermore, this agent reduces angiogenesis and metastasis in a human xenograft tumor model. The Jak2 inhibitor suppresses the growth of human solid tumor xenografts harboring persistent Stat3 activity.
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참조 |
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| 방법 | 바이오마커 | 이미지 | 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 |
(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)
| NCT 번호 | 모집 | 조건 | 스폰서/협력자 | 시작일 | 단계 |
|---|---|---|---|---|---|
| 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 |