计算溶液所需的质量、体积或浓度。
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
NSC12 是 FGF2 的细胞外陷阱，与 FGF2 结合并干扰其与 FGFR1 的相互作用。NSC12 在体外和体内均能抑制 FGF 依赖性不同肿瘤细胞的增殖，且无全身毒性作用。
Information
NSC12 NSC12 (NSC 172285) is an orally available pan-FGF trap able to inhibit FGF2/FGFR interaction and endowed with promising antitumor activity.
Targets
FGF3 (Cell-free assay); FGF8b (Cell-free assay); FGF22 (Cell-free assay); FGF20 (Cell-free assay); FGF2/FGFR (Cell-free assay) 16447,15.9 μM(Kd); 18.9 μM(Kd) ;26.8 μM(Kd); 29.4 μM(Kd); 30 μM
In vitro
NSC12 inhibits FGF-dependent tumor growth, angiogenesis, and metastases. NSC12 does not affect FGF2/heparin interaction, whereas it inhibits the binding of FGF2 to the immobilized receptor (ID50 ∼30 μM). NSC12 interferes with FGF2/FGFR1 interaction without affecting the ability of the growth factor to interact with heparin or HSPGs. NSC12 also binds immobilized FGF3, FGF4, FGF6, FGF8, FGF16, FGF18, FGF20, and FGF22 with Kd values ranging between ∼16 and ∼120 μM. NSC12 may act as a multi-FGF trap by interacting with all members of the canonical FGF subfamilies. NSC12 hampers FGF23-mediated FGFR1 activation in Klotho-expressing Chinese hamster ovary (CHO) cells. Treatment with NSC12 causes the reduction of the S phase of the cell cycle in all tumor cell lines but LLC cells, in which an accumulation in the S phase is observed. NSC12 inhibits FGFR1, FGFR2, FGFR3, and FGFR4 phosphorylation in CHO cell transfectants. NSC12 inhibits the proliferation of various FGF-dependent murine and human cancer cell lines with no inhibitory effect on HCC827 cancer cells that harbor a tumor-driving mutation of the EGFR TK domain and on FGF-independent cancer cell lines.
In vivo
Parenteral and oral delivery of NSC12 inhibits FGFR activation, tumor growth, angiogenesis, and metastasis in FGF-dependent murine and human tumor models. NSC12 causes a significant decrease of tumor weight, tumor cell FGFR1 phosphorylation and proliferation, and tumor CD31+ neovascularization at all the doses tested in the animal models.
Cell Research(from reference)
Cell lines：KATO Ⅲ cells
Concentrations：1.0 or 3.0 μM
Incubation Time：72 h
规格
英文别名
Pregn-5-ene-3,20-diol, 21-(2-hydroxy-1,1,1,3,3,3-hexafluoro-2-propyl)- | 102586-30-1 | 21-(Hydroxy(bistrifluoromethyl)methyl)pregnane-3,20-diol | 4,4,4-trifluoro-1-[(8S,9S,10R,13S,14S,17S)-3-hydroxy-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cy
规格或纯度
10mM in DMSO
英文名称
NSC12
生化机理
NSC12 （NSC 172285）是一种口服泛生长因子诱捕剂，能够抑制 FGF2/FGFR 相互作用，具有良好的抗肿瘤活性。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
PubChem SID
分子类型
小分子
IUPAC Name
4,4,4-trifluoro-1-[(8S,9S,10R,13S,14S,17S)-3-hydroxy-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl]-3-(trifluoromethyl)butane-1,3-diol
INCHI
1S/C24H34F6O3/c1-20-9-7-14(31)11-13(20)3-4-15-16-5-6-18(21(16,2)10-8-17(15)20)19(32)12-22(33,23(25,26)27)24(28,29)30/h3,14-19,31-33H,4-12H2,1-2H3/t14?,15-,16-,17-,18+,19?,20-,21-/m0/s1
InChi Key
OHKBOEWLASAFLW-DRPHTYIMSA-N
Smiles
CC12CCC3C(C1CCC2C(CC(C(F)(F)F)(C(F)(F)F)O)O)CC=C4C3(CCC(C4)O)C
Isomeric SMILES
C[C@]12CC[C@H]3[C@H]([C@@H]1CC[C@@H]2C(CC(C(F)(F)F)(C(F)(F)F)O)O)CC=C4[C@@]3(CCC(C4)O)C
分子量
484.52
Reaxy-Rn
29542218
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=29542218&ln=
技术文档
高级数据
三维结构
交互式化学结构模型
产品属性
| ALogP | 4.884 |
|---|---|
| HBD Count | 2 |
| Rotatable Bond | 5 |
化学和物理性质
DMSO(mg / mL) Max Solubility
96
DMSO(mM) Max Solubility
198.1342359
Water(mg / mL) Max Solubility
＜1
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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溶液计算器
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