FGTI-2734

COA

级别和纯度:

≥99%

CAS编号: 1247018-19-4
分子式: C₂₆H₃₁FN₆O₂S
分子量: 510.63
PubChem编号: 49783195

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货号 (SKU)	包装规格	是否现货
F649320-5mg	5mg	期货
F649320-10mg	10mg	期货
F649320-25mg	25mg	期货
F649320-50mg	50mg	期货
F649320-100mg	100mg	期货

查看相关系列

Amino Acid/Protein Metabolism (4559) Farnesyl Transferase (28) Metabolic Enzyme/Protease (4889)

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基本描述

规格或纯度	≥99%
英文名称	FGTI-2734
生化机理	FGTI-2734 是一种 RAS C--terminal mimetic 双法尼基转移酶（FT）和香叶基转移酶-1（GGT-1）抑制剂，FT 和 GGT-1 的 IC 50 s 分别为 250 nM 和 520 nM。FGTI-2734 可阻止 KRAS 的膜定位，从而解决 KRAS 的膜定位问题。
储存温度	2-8°C储存
运输条件	冰袋运输
作用类型	抑制剂
产品介绍	FGTI-2734 is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC 50 s of 250 nM and 520 nM for FT and GGT-1, respectively. FGTI-2734 can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors In Vitro FGTI-2734 (1-30 μM; 72 hours) induces CASPASE-3 and PARP cleavage in MiaPaCa2, L3.6pl and Calu6 cells. FGTI-2734 (3-30 μM; 72 hours) inhibits both protein prenylation of HDJ2, RAP1A, KRAS and NRAS. FGTI-2734 inhibits KRAS membrane localization in RAS-transformed murine NIH3T3 cells and in mutant KRAS human cancer cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Apoptosis AnalysisCell Line: MiaPaCa2, L3.6pl and Calu6 cells Concentration: 1, 3, 10, 30 μM Incubation Time: 72 hours Result: Induced CASPASE-3 and PARP cleavage in MiaPaCa2, L3.6pl and Calu6 cells. Western Blot AnalysisCell Line: KRAS, HRAS, and NRAS-transformed NIH3T3 cells Concentration: 3, 10, 30 μM Incubation Time: 72 hours Result: Inhibited both protein prenylation of HDJ2, RAP1A, KRAS and NRAS. In Vivo FGTI-2734 (intraperitoneally; 100 mg/kg/daily for 18 to 25 days) only inhibits tumor growth in mutant KRAS-dependent tumors but not in mutant KRAS-independent tumors . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male SCID-bg mice following injection of MiaPaCa2, L3.6pl, Calu6, A549, H460 and DLD1 cancer cells Dosage: 100 mg/kg Administration: Intraperitoneally; daily; for 18 to 25 days Result: Inhibited tumor growth in mutant KRAS-dependent tumors. Form:Solid IC50& Target:IC50: 250 nM (FT) and 520 nM (GGT-1)
纯度	≥99%

关联靶点（人）

FNTA Tclin Protein farnesyltransferase (3470 活性数据)

点击查看靶蛋白信息： FNTA

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

FNTA Tclin Geranylgeranyl transferase type I (851 活性数据)

点击查看靶蛋白信息： FNTA

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

关联靶点（其它种属）

Fnta Geranylgeranyl transferase type 1 (44 活性数据)

点击查看靶蛋白信息： Fnta

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	N-[2-[4-cyano-2-fluoro-N-[(3-methylimidazol-4-yl)methyl]anilino]ethyl]-N-(cyclohexylmethyl)pyridine-2-sulfonamide
INCHI	1S/C26H31FN6O2S/c1-31-20-29-17-23(31)19-32(25-11-10-22(16-28)15-24(25)27)13-14-33(18-21-7-3-2-4-8-21)36(34,35)26-9-5-6-12-30-26/h5-6,9-12,15,17,20-21H,2-4,7-8,13-14,18-19H2,1H3
InChi Key	BXNRVJLIEMQDOL-UHFFFAOYSA-N
Smiles	CN1C=NC=C1CN(CCN(CC2CCCCC2)S(=O)(=O)C3=CC=CC=N3)C4=C(C=C(C=C4)C#N)F
Isomeric SMILES	CN1C=NC=C1CN(CCN(CC2CCCCC2)S(=O)(=O)C3=CC=CC=N3)C4=C(C=C(C=C4)C#N)F
PubChem CID	49783195
分子量	510.63

化学和物理性质

溶解性	DMSO : 50 mg/mL (97.92 mM; Need ultrasonic)
分子量	510.600 g/mol
XLogP3	4.000
氢键供体数Hydrogen Bond Donor Count	0
氢键受体数Hydrogen Bond Acceptor Count	8
可旋转键计数Rotatable Bond Count	10
精确质量Exact Mass	510.221 Da
单同位素质量Monoisotopic Mass	510.221 Da
拓扑极表面积Topological Polar Surface Area	104.000 Å²
重原子数Heavy Atom Count	36
形式电荷Formal Charge	0
复杂度Complexity	839.000
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	0
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

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