2. Apoptosis Protein Tyrosine Kinase/RTK Cell Cycle/DNA Damage Epigenetics
  3. Apoptosis FGFR HDAC
  4. HDAC-IN-50

HDAC-IN-50 是一种有效的，具有口服活性的 FGFR 和 HDAC 双重抑制剂，对 FGFR1, FGFR2, FGFR3, FGFR4, HDAC1, HDAC2, HDAC6, HDAC8 的IC50 值分别为 0.18, 1.2, 0.46, 1.4, 1.3, 1.6, 2.6, 13 nM。HDAC-IN-50 诱导细胞凋亡(Apoptosis) 和细胞周期停滞在 G0/G1 期。HDAC-IN-50 降低 pFGFR1、pERK、pSTAT3 的表达。HDAC-IN-50 具有抗肿瘤活性。

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HDAC-IN-50 Chemical Structure

HDAC-IN-50 Chemical Structure

CAS No. : 2653339-26-3

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HDAC-IN-50 相关抗体

Top Publications Citing Use of Products

查看 FGFR 亚型特异性产品:

查看所有亚型
FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

查看 HDAC 亚型特异性产品:

查看所有亚型
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HDAC-IN-50 is a potent and orally active FGFR and HDAC dual inhibitor with IC50 values of 0.18, 1.2, 0.46, 1.4, 1.3, 1.6, 2.6, 13 nM for FGFR1, FGFR2, FGFR3, FGFR4, HDAC1, HDAC2, HDAC6, HDAC8, respectively. HDAC-IN-50 induces Apoptosis and cell cycle arrest at G0/G1 phase. HDAC-IN-50 decreases the expression of pFGFR1, pERK, pSTAT3. HDAC-IN-50 shows anti-tumor activity[1].

IC50 & Target[1]

FGFR1

0.18 nM (IC50)

FGFR2

1.2 nM (IC50)

FGFR3

0.46 nM (IC50)

FGFR4

1.4 nM (IC50)

HDAC1

1.3 nM (IC50)

HDAC2

1.6 nM (IC50)

HDAC6

2.6 nM (IC50)

HDAC8

13 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A2780 IC50
0.04 μM
Compound: 10e
Antiproliferative activity against human A2780 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human A2780 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 36449947]
HCT-116 IC50
0.82 μM
Compound: 10e
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 36449947]
Jurkat IC50
15.14 μM
Compound: 10e
Antiproliferative activity against human Jurkat cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human Jurkat cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 36449947]
K562 IC50
2.46 μM
Compound: 10e
Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 36449947]
KATO III stomach cancer cell line IC50
0.0008 μM
Compound: 10e
Antiproliferative activity against human KATO III stomach cancer cell line assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human KATO III stomach cancer cell line assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 36449947]
SNU-16 IC50
0.0007 μM
Compound: 10e
Antiproliferative activity against human SNU-16 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human SNU-16 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 36449947]
体外研究
(In Vitro)

HDAC-IN-50 (compound 10e) (0.1, 1, 10, 100 nM; 12-84 h) 以时间和剂量依赖性方式诱导细胞凋亡和细胞周期停滞在 G0/G1 期[1]< /sup>。
HDAC-IN-50 (0, 1.25, 2.5, 5 µM for HCT116 cells, 0, 1, 10, 100 nM for SNU-16 cells; 36 h) 以剂量依赖性方式降低 pFGFR1、pERK、pSTAT3 的表达 [1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

HDAC-IN-50 相关抗体:

Cell Proliferation Assay[1]

Cell Line: HCT116, SNU-16, KATO III, A2780, K562, Jurkat cells
Concentration: 0-30 µM
Incubation Time: 72 h
Result: Showed antiproliferative activities with IC50s of 0.82, 0.0007, 0.0008, 0.04, 2.46, 15.14 µM for HCT116, SNU-16, KATO III, A2780, K562, Jurkat cells, respectively.

Cell Cycle Analysis[1]

Cell Line: SNU-16 cells
Concentration: 0.1, 1, 10, 100 nM
Incubation Time: 12, 24, 36 h
Result: Induced cell cycle arrest at G0/G1 phase in a time and dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: SNU-16 cells
Concentration: 0.1, 1, 10, 100 nM
Incubation Time: 36, 48, 60, 72, 84 h
Result: Induced apoptosis with the apoptotic rate increased 30.8% and 49.6% at 10, 100 nM, respectively.

Western Blot Analysis[1]

Cell Line: HCT116, SNU-16 cells
Concentration: 0, 1.25, 2.5, 5 µM for HCT116 cells, 0, 1, 10, 100 nM for SNU-16 cells
Incubation Time: 36 h
Result: Reduced the expression of pFGFR1, pERK, pSTAT3 in a dose-dependent manner.
体内研究
(In Vivo)

HDAC-IN-50 (15、30 mg/kg；口服；每日一次，持续 18 天) 在小鼠体内显示出抗肿瘤活性[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c nude mice (HCT116 xenograft model)[1]
Dosage: 15, 30 mg/kg
Administration: P.o.; daily for 18 days
Result: Inhibited the tumor growth and downregulated the expression of pSTAT3, pFGFR1, increased the expression of Ac-H3.
分子量

575.70

Formula

C31H41N7O4
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

HDAC-IN-50 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HDAC-IN-502653339-26-3ApoptosisFGFRHDACFibroblast growth factor receptorHistone deacetylasesapoptosisG0/G1pFGFR1pERKpSTAT3antiproliferativeanti-tumorHCT116SNU-16 cellsInhibitorinhibitorinhibit

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