Determine the necessary mass, volume, or concentration for preparing a solution.
| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
|---|
이 등급을 선택하는 이유
Moligand™,≥98% Moligand™ 최소한의 기준선 간섭이 필요한 민감한 크로마토그래피 및 분석 워크플로우용.
보관 및 배송
Protected from light,Store at -20°C,Argon charged Ice chest + Ice pads 출고. 정확한 사양은 로트별 COA를 확인하세요.
품질 문서
SDS, COA, 데이터시트, 사양서를 다운로드할 수 있습니다. 로트별 COA는 로트 번호 조회를 통해 확인할 수 있습니다.
문헌적 근거
크로마토그래피, 유기 합성 및 교차 커플링 반응 분야의 동료 심사 논문 0편에서 인용되었습니다.
개요
EHT 1610 is a potent inhibitor of DYRK , with IC 50 s of 0.36 nM ( DYRK1A ), 0.59 nM ( DYRK1B ), respectively. EHT 1610 exhibits antileukemia effect, regulates cell cycle and induces cell apoptosis.
In Vitro
EHT 1610 induces apoptosis of primary ALL cells that were resistant to cytarabine. EHT 1610 dose-dependently induces apoptosis in B- and T-cell lines and primary human pediatric. EHT 1610 (; 72 h) inhibits DYRK1A, results loss of DYRK1A-mediated FOXO1 and STAT3 signaling, leading to preferential cell death in leukemic B cells. EHT 1610 (2.5-10 μM; 4-5 h) inhibits phosphorylation of FOXO1, STAT3 and cyclin D3, thus regulates late cell-cycle progression, mitochondrial ROS and DNA damage, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: MHH-CALL-4 cells Concentration: 0, 2.5, 5, 10 μM Incubation Time: 4, 5 hours Result: Reduced p-cyclin D3 (Thr283), and p-FOXO1 protein level in a dose-dependent manner.
In Vivo
EHT 1610 (20 mg/kg/d; i.p.; twice a day; 3 weeks) shows antileukemia activity against in leukemic aggressive model in mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Xenograft models of B-ALL in mice (12-14 weeks old)Dosage: 20 mg/kg Administration: Intraperitoneal injection; twice a day, 5 days on, 2 days off; 3 weeks Result: Reduced leukemic burden by approximately 8% and conferred a modest survival advantage.
Form:Solid
IC50& Target:IC50: 0.36 nM (DYRK1A), 0.59 nM (DYRK1B)
사양
사양 및 순도
Moligand™,≥98%
생화학 및 생리적 메커니즘
EHT 1610 is a potent inhibitor of DYRK , with IC 50 s of 0.36 nM ( DYRK1A ), 0.59 nM ( DYRK1B ), respectively. EHT 1610 exhibits antileukemia effect, regulates cell cycle and induces cell apoptosis- .
보관 조건
Protected from light,Store at -20°C,Argon charged
배송
Ice chest + Ice pads
이 제품은 콜드 체인 배송이 필요합니다.지상 및 기타 경제 서비스는 사용할 수 없습니다.
등급
Moligand™
작업 유형
INHIBITOR
순수함
≥98%
이름과 식별자
정식 스마일
COC1=CC(=C(C=C1)NC2=NC=NC3=C2C4=C(C=C3)N=C(S4)C(=N)OC)F
IUPAC Name
methyl 9-(2-fluoro-4-methoxyanilino)-[1,3]thiazolo[5,4-f]quinazoline-2-carboximidate
InChIKey
RYBNARZBIXTFJS-UHFFFAOYSA-N
INCHI
1S/C18H14FN5O2S/c1-25-9-3-4-11(10(19)7-9)23-17-14-12(21-8-22-17)5-6-13-15(14)27-18(24-13)16(20)26-2/h3-8,20H,1-2H3,(H,21,22,23)
이성체 SMILES
COC1=CC(=C(C=C1)NC2=NC=NC3=C2C4=C(C=C3)N=C(S4)C(=N)OC)F
대체 CAS
1425945-63-6
MeSH 용어
EHT 1610
분자량
383.40
문서
📋 안전 데이터 시트(SDS)
위험성, 취급, 보관 및 규제 준수를 포괄하는 종합 문서.
<<<<<<< HEAD SDS 다운로드 → ======= SDS 다운로드 → >>>>>>> release248-p3고급 데이터
Taxonomic Classification
Taxonomy Tree
- Kingdom Organic compounds
- Superclass Organoheterocyclic compounds
- 분류 Diazanaphthalenes
- Subclass Benzodiazines
- Level5 Quinazolines
- Level6 Quinazolinamines
- Level5 Quinazolines
- Subclass Benzodiazines
- 분류 Diazanaphthalenes
- Superclass Organoheterocyclic compounds
| Kingdom | Organic compounds |
|---|---|
| Superclass | Organoheterocyclic compounds |
| 분류 | Diazanaphthalenes |
| Subclass | Benzodiazines |
| Intermediate Tree Nodes | Quinazolines |
| Direct Parent | Quinazolinamines |
| Alternative Parents | Benzothiazoles Methoxyanilines Anisoles Phenoxy compounds Methoxybenzenes Alkyl aryl ethers Aminopyrimidines and derivatives Fluorobenzenes Aryl fluorides Imidolactams Thiazoles Heteroaromatic compounds Carboximidic acids and derivatives Azacyclic compounds Amines Organofluorides Hydrocarbon derivatives |
| Molecular Framework | Aromatic heteropolycyclic compounds |
| Substituents | Quinazolinamine - 1,3-benzothiazole - Methoxyaniline - Phenoxy compound - Anisole - Methoxybenzene - Aniline or substituted anilines - Phenol ether - Alkyl aryl ether - Aminopyrimidine - Fluorobenzene - Halobenzene - Aryl fluoride - Aryl halide - Monocyclic benzene moiety - Imidolactam - Benzenoid - Pyrimidine - Heteroaromatic compound - Azole - Thiazole - Azacycle - Ether - Carboximidic acid derivative - Organohalogen compound - Hydrocarbon derivative - Organic oxygen compound - Amine - Organofluoride - Organonitrogen compound - Organooxygen compound - Organic nitrogen compound - Aromatic heteropolycyclic compound |
| 설명 | This compound belongs to the class of organic compounds known as quinazolinamines. These are heterocyclic aromatic compounds containing a quianazoline moiety substituted by one or more amine groups. |
| External Descriptors | Not available |
3D 구조
상호 작용 화학 구조 모델
관련 대상(인간)
DYRK1B Tchem Dual specificity tyrosine-phosphorylation-regulated kinase 1B (3 Activities)
DYRK2 Tchem Dual specificity tyrosine-phosphorylation-regulated kinase 2 (1 Activities)
| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
|---|
DYRK3 Tchem Dual specificity tyrosine-phosphorylation-regulated kinase 3 (1 Activities)
| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
|---|
DYRK1A Tchem Dual specificity tyrosine-phosphorylation-regulated kinase 1A (4 Activities)
| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
|---|
CLK1 Tchem Dual specificity protein kinase CLK1 (1 Activities)
| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
|---|
GSK3A Tclin Glycogen synthase kinase-3 alpha (1 Activities)
| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
|---|
ABL1 Tclin Tyrosine-protein kinase ABL (18331 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
CSNK2A1 Tchem Casein kinase II alpha (3512 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
DAPK3 Tchem Death-associated protein kinase 3 (2108 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
NQO2 Tchem Quinone reductase 2 (885 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
MAPK14 Tchem MAP kinase p38 alpha (12866 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
GSK3B Tclin Glycogen synthase kinase-3 beta (11785 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
MAP2K6 Tchem Dual specificity mitogen-activated protein kinase kinase 6 (1284 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
FGFR2 Tclin Fibroblast growth factor receptor 2 (3405 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
FGFR1 Tclin Fibroblast growth factor receptor 1 (9149 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
STK3 Tchem Serine/threonine-protein kinase MST2 (3069 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
CSNK1D Tchem Casein kinase I delta (4546 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
CAMK2B Tchem CaM kinase II beta (1626 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
SRC Tclin Tyrosine-protein kinase SRC (10310 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
CHEK2 Tchem Serine/threonine-protein kinase Chk2 (4015 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
AKT3 Tchem Serine/threonine-protein kinase AKT3 (3157 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
PIM1 Tchem Serine/threonine-protein kinase PIM1 (9629 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
RPS6KA5 Tchem Ribosomal protein S6 kinase alpha 5 (3355 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
RPS6KA1 Tchem Ribosomal protein S6 kinase alpha 1 (2796 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
CSNK1E Tclin Casein kinase I epsilon (1412 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
CAMK4 Tbio CaM kinase IV (2116 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
GSK3A Tclin Glycogen synthase kinase-3 alpha (3764 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
MAP2K4 Tchem Dual specificity mitogen-activated protein kinase kinase 4 (1051 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
MAPK13 Tchem MAP kinase p38 delta (2605 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
MAPKAPK2 Tchem MAP kinase-activated protein kinase 2 (4814 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
DAPK1 Tchem Death-associated protein kinase 1 (1664 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
MAPK9 Tchem c-Jun N-terminal kinase 2 (4655 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
MAPK10 Tchem c-Jun N-terminal kinase 3 (3396 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
CAMK2D Tchem CaM kinase II delta (2813 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
CDK2 Tchem Cyclin-dependent kinase 2 (9050 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
MAP3K10 Tchem Mitogen-activated protein kinase kinase kinase 10 (401 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
MAP3K9 Tchem Mitogen-activated protein kinase kinase kinase 9 (945 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
DYRK1A Tchem Dual-specificity tyrosine-phosphorylation regulated kinase 1A (6484 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
MAPK8 Tchem c-Jun N-terminal kinase 1 (5038 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
PHKG2 Tchem Phosphorylase kinase gamma subunit 2 (2281 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
CSNK2A2 Tchem Casein kinase II alpha (prime) (1587 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
MAP2K7 Tchem Dual specificity mitogen-activated protein kinase kinase 7 (1145 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
AURKA Tchem Serine/threonine-protein kinase Aurora-A (10240 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
GAK Tchem Serine/threonine-protein kinase GAK (1150 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
AAK1 Tchem Adaptor-associated kinase (1053 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
PLK4 Tchem Serine/threonine-protein kinase PLK4 (1882 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
STK17B Tchem Serine/threonine-protein kinase 17B (773 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
STK10 Tchem Serine/threonine-protein kinase 10 (2119 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
EPHA2 Tclin Ephrin type-A receptor 2 (3499 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
TTK Tchem Dual specificity protein kinase TTK (2978 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
CLK1 Tchem Dual specificty protein kinase CLK1 (2189 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
CLK2 Tchem Dual specificity protein kinase CLK2 (3942 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
CLK3 Tchem Dual specificity protein kinase CLK3 (2711 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
BMX Tchem Tyrosine-protein kinase BMX (1995 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
NEK2 Tchem Serine/threonine-protein kinase NEK2 (3514 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
EPHA5 Tchem Ephrin type-A receptor 5 (1056 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
관련 대상(비인간)
Mapk1 MAP kinase ERK2 (650 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
Fgfr3 Fibroblast growth factor receptor 3 (21 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
HT-22 (3261 Activities)
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
작용 메커니즘
인증서(CoA, COO, BSE/TSE 및 분석 차트)
C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:
화학 및 물리적 특성
| 용해성 | DMSO : 5 mg/mL (13.04 mM; Need ultrasonic) |
|---|---|
| 분자량 | 383.400 g/mol |
| XLogP3 | 4.200 |
| Hydrogen Bond Donor Count | 2 |
| Hydrogen Bond Acceptor Count | 9 |
| Rotatable Bond Count | 5 |
| Exact Mass | 383.085 Da |
| Monoisotopic Mass | 383.085 Da |
| Topological Polar Surface Area | 121.000 Ų |
| Heavy Atom Count | 27 |
| Formal Charge | 0 |
| Complexity | 544.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| The total count of all stereochemical bonds | 0 |
| Covalently-Bonded Unit Count | 1 |
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