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

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.

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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 Related Antibodies

Top Publications Citing Use of Products

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FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

  • Biological Activity

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Description

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)

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]
In Vitro

HDAC-IN-50 (compound 10e) (0.1, 1, 10, 100 nM; 12-84 h) induces apoptosis and cell cycle arrest at G0/G1 phase in a time and dose-dependent manner[1].
HDAC-IN-50 (0, 1.25, 2.5, 5 µM for HCT116 cells, 0, 1, 10, 100 nM for SNU-16 cells; 36 h) decreases the expression of pFGFR1, pERK, pSTAT3 in a dose-dependent manner[1].

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

HDAC-IN-50 Related Antibodies

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.
In Vivo

HDAC-IN-50 (15, 30 mg/kg; p.o.; daily for 18 days) shows anti-tumor activity in mouse[1].
Pharmacokinetic Parameters of HDAC-IN-50 in female Sprague–Dawley (SD) rats[1].

dose (mg/kg) administration route T1/2 (h) Tmax (h) Cmax (ng/mL) AUC0-∞ (h·ng/mL) CL (mL/min/kg) Vss (mL/kg) F %
2 IV 0.98± 0.12 0.08 1116.63 ± 320.45 424.88 ± 89.56 80.64 ± 15.59 2788.87 ± 765.11
5 IP 1.83 ± 0.06 2 101.57 ± 23.05 491.25 ± 84.18 43.83
30 PO 0.77 ± 0.04 4 442.53 ± 46.33 1557.12 ± 355.61 24.83
Female Sprague-Dawley (SD) rats, 5 mg/kg iv; 5 mg/kg ip; 30 mg/kg p.o.[1]

MedChemExpress (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.
Molecular Weight

575.70

Formula

C31H41N7O4
CAS No.
SMILES

O=C(CCCCCCN1N=CC(C2=NC3=C(N=C2)C=CC(N(CCNC(C)C)C4=CC(OC)=CC(OC)=C4)=C3)=C1)NO
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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HDAC-IN-50 Related Classifications

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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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