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NSC-370284

    级别和纯度:
  • ≥96%
  • CAS编号: 116409-29-1
  • 分子式: C21H25NO6
  • 分子量: 387.43
  • PubChem编号: 340208
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货号 (SKU) 包装规格 是否现货 价格 数量
N646601-5mg
5mg 期货 Stock Image
N646601-10mg
10mg 期货 Stock Image
N646601-25mg
25mg 期货 Stock Image
N646601-50mg
50mg 期货 Stock Image
N646601-100mg
100mg 期货 Stock Image

基本描述

英文别名 NCI60_003410 | AKOS024282084 | 6-[1-pyrrolidinyl-(3,4,5-trimethoxyphenyl)methyl]-1,3-benzodioxol-5-ol | 6-(1-Pyrrolidinyl(3,4,5-trimethoxyphenyl)methyl)-1,3-benzodioxol-5-ol | 6-[(3,5-Trimethoxyphenyl)-1-pyrrolidinylmethyl]-1,3-benzodioxol-5-ol | {6-[(3,4
规格或纯度 ≥96%
英文名称 NSC-370284
生化机理 NSC-370284 是十-十一转位 1(TET1)和 5-羟甲基胞嘧啶(5hmC)的选择性抑制剂。NSC-370284 通过靶标 STAT3/5 显著抑制 TET1 的表达水平。
储存温度 -20°C储存
运输条件 超低温冰袋运输
作用类型 抑制剂
产品介绍


NSC-370284 is a selective inhibitor of ten-eleven translocation 1 ( TET1 ) and 5-hydroxymethylcytosine ( 5hmC ). NSC-370284 significantly inhibits the level of TET1 expression via targets STAT3/5

In Vitro

NSC-370284 (0-500 nM; 24 h or 48 h) inhibits the viability of MONOMAC-6, THP-1, KOCL-48 and KASUMI-1 acute myeloid leukemia (AML) cells via targeting STAT3/5. NSC-370284 significantly down-regulates the level of TET1 transcription. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: AML cell lines including MONOMAC-6, THP-1, KOCL-48, and KASUMI-1. Concentration: 0, 25, 50, 200 or 500 nM. Incubation Time: 24 h or 48 h. Result: Showed inhibitory for AML cells viability and TET1 transcription.

In Vivo

NSC-370284 (2.5 mg/kg; i.p., once daily for 10 days) improves the pathological morphologies in peripheral blood (PB), bone marrow (BM), spleen, and liver tissues in MLL-AF9 acute myeloid leukemia (AML) mice model . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: C57BL/6 (CD45.2) and B6.SJL (CD45.1) mice . Dosage: 2.5 mg/kg. Administration: Intraperitoneal injection, once daily, for 10 days. Result: Significantly inhibited MLL-AF9 induced AML in secondary bone marrow transplantation (BMT) recipient mice.

Form:Solid

IC50& Target:STAT3 STAT5 TET1

纯度 ≥96%

关联靶点(人)

P4HB Tchem 蛋白质二硫键异构酶(Protein disulfide-isomerase) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
A498 (42825 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ACHN (49357 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CAKI-1 (44928 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CCRF-CEM (65223 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
COLO 205 (50209 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DU-145 (51482 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HL-60 (67320 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HT-29 (80576 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
K562 (73714 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
KM12 (47707 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
M14 (47487 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MCF7 (126967 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MOLT-4 (49676 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OVCAR-3 (48710 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OVCAR-4 (44535 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OVCAR-5 (45555 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OVCAR-8 (47708 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PC-3 (62116 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RPMI-8226 (44974 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SF-295 (48000 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SK-MEL-2 (46422 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SK-MEL-28 (48833 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SK-MEL-5 (47095 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SK-OV-3 (52876 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SN12C (47755 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SNB-19 (46794 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
TK-10 (45540 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
U-251 (51189 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
U-87 MG (3946 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
UACC-257 (46019 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
UACC-62 (47335 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
UO-31 (46270 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
786-0 (47912 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
A549 (127892 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
NCI/ADR-RES (33767 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
T47D (39041 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
EKVX (44102 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
NCI-H322M (45589 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HCC 2998 (41480 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HCT-116 (91556 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HOP-92 (41141 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
IGROV-1 (47897 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
LOX IMVI (44321 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HOP-62 (47048 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MDA-MB-435 (38290 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MDA-N (28205 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Malme-3M (44254 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MDA-MB-231 (73002 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SNB-75 (44215 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
NCI-H226 (44470 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

作用机制

作用机制 Action Type target ID Target Name Target Type Target Organism Binding Site Name 参考文献

名称和识别符

分子类型 小分子
IIUPAC Name 6-[pyrrolidin-1-yl-(3,4,5-trimethoxyphenyl)methyl]-1,3-benzodioxol-5-ol
INCHI 1S/C21H25NO6/c1-24-18-8-13(9-19(25-2)21(18)26-3)20(22-6-4-5-7-22)14-10-16-17(11-15(14)23)28-12-27-16/h8-11,20,23H,4-7,12H2,1-3H3
InChi Key QCXGNLZKUHBIHD-UHFFFAOYSA-N
Smiles COC1=CC(=CC(=C1OC)OC)C(C2=CC3=C(C=C2O)OCO3)N4CCCC4
Isomeric SMILES COC1=CC(=CC(=C1OC)OC)C(C2=CC3=C(C=C2O)OCO3)N4CCCC4
关联CAS 116409-29-1
PubChem CID 340208
NSC Number 370284
分子量 387.43

化学和物理性质

溶解性 DMSO : 100 mg/mL (258.11 mM; Need ultrasonic)
分子量 387.400 g/mol
XLogP3 3.300
氢键供体数Hydrogen Bond Donor Count 1
氢键受体数Hydrogen Bond Acceptor Count 7
可旋转键计数Rotatable Bond Count 6
精确质量Exact Mass 387.168 Da
单同位素质量Monoisotopic Mass 387.168 Da
拓扑极表面积Topological Polar Surface Area 69.600 Ų
重原子数Heavy Atom Count 28
形式电荷Formal Charge 0
复杂度Complexity 487.000
同位素原子数Isotope Atom Count 0
定义的原子立体中心计数Defined Atom Stereocenter Count 0
未定义的原子立体中心计数Undefined Atom Stereocenter Count 1
定义的键立体中心计数Defined Bond Stereocenter Count 0
未定义的键立体中心计数Undefined Bond Stereocenter Count 0
所有立体化学键的总数The total count of all stereochemical bonds 0
共价键合单元计数Covalently-Bonded Unit Count 1

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

溶液计算器