2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. HDAC Apoptosis
  4. Nanatinostat TFA

Nanatinostat (CHR-3996) TFA is a potent, class I selective and orally active HDAC inhibitor with IC50s of 3 nM, 4 nM, and 7 nM for HDAC1, HDAC2, and HDAC3, respectively. Nanatinostat TFA has low activity against HDAC5 (IC50 of 200 nM) and HDAC6 (IC50 of 2100 nM). Nanatinostat TFA induces apoptosis in myeloma cells. Nanatinostat TFA has potent anticancer effects, such as myeloma, advanced solid tumours and colorectal cancer.

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Nanatinostat TFA

Nanatinostat TFA Chemical Structure

CAS No. : 1256448-48-2

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Nanatinostat TFA Related Antibodies

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

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Description

Nanatinostat (CHR-3996) TFA is a potent, class I selective and orally active HDAC inhibitor with IC50s of 3 nM, 4 nM, and 7 nM for HDAC1, HDAC2, and HDAC3, respectively. Nanatinostat TFA has low activity against HDAC5 (IC50 of 200 nM) and HDAC6 (IC50 of 2100 nM). Nanatinostat TFA induces apoptosis in myeloma cells. Nanatinostat TFA has potent anticancer effects, such as myeloma, advanced solid tumours and colorectal cancer[1][2][3].

IC50 & Target[1]

HDAC1

3 nM (IC50)

HDAC2

4 nM (IC50)

HDAC3

7 nM (IC50)

HDAC

8 nM (IC50)

HDAC5

200 nM (IC50)

HDAC6

2100 nM (IC50)

In Vitro

Nanatinostat (CHR-3996) (0.0001-1 μM; 48 hours) TFA inhibits the proliferation of myeloma cell lines, with LC50 values ranging from 30.3-97.6 nM in different cell lines[2].
Nanatinostat (250-100 nM; 8-48 hours)TFA induces apoptosis and increases the level of acetylated H3K9 in H929 and RPMI-8226 myeloma cell lines[2].
Nanatinostat (0-200 nM; 24 hours) TFA reduces the levels of IL-6 and VEGF secreted by bone marrow stromal cells in the co-culture system of bone marrow stromal cells and myeloma cells[2].
Nanatinostat (250 nM and 100 nM; 48 hours) TFA arrests the cell cycle at the G0/G1 phase in H929 and RPMI-8226 myeloma cell lines[2].

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

Nanatinostat TFA Related Antibodies

Cell Viability Assay[2]

Cell Line: H929, RPMI-8226, KMS11, LP-1, MM1-S cells
Concentration: 0.0001 μM, 0.001 μM, 0.01 μM, 0.1 μM, 1 μM
Incubation Time: 48 hours
Result: The cell viability decreased.

Apoptosis Analysis[2]

Cell Line: H929 and RPMI-8226 myeloma cell lines
Concentration: 100 nM (RPMI-8226 cells), 250 nM (H929 cells)
Incubation Time: 8 hours, 24 hours, 48 hours
Result: The percentage of apoptotic cells increased, with an increase in both early and late apoptotic cells.

Cell Cycle Analysis[2]

Cell Line: H929 and RPMI-8226 myeloma cell lines
Concentration: 100 nM (RPMI-8226 cells), 250 nM (H929 cells)
Incubation Time: 48 hours
Result: The cell cycle was arrested at the G0/G1 phase.

Western Blot Analysis[2]

Cell Line: H929 and RPMI-8226 myeloma cell lines
Concentration: 100 nM (RPMI-8226 cells), 250 nM (H929 cells)
Incubation Time: 8 hours, 24 hours, 48 hours
Result: The pro-apoptotic DNase Endonuclease G and p53 downstream mediator Noxa were up-regulated, and caspase 9 was cleaved.
In Vivo

Nanatinostat (50 mg/kg; orally administered; once daily; for 14 days) TFA can almost completely inhibit tumor growth in the female CrTac:NCr-Fox1ν mouse HCT116 tumor xenograft model[1].
Nanatinostat (25-50 mg/kg; orally administered; once daily; for 19 days) TFA can significantly reduce tumor volume in a dose-dependent manner in the female BALB/c nude mouse LoVo human colon xenograft model[1].
Nanatinostat (30 mg/kg; orally administered; once daily; for 28 days) TFA can effectively inhibit tumor growth in the NOD/SCID IL2R gammanull mouse myeloma model[2].

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

Animal Model: Female CrTac:NCr-Fox1(nu) mice (6-8 weeks old; inoculated bilaterally sc with 2 million human HCT116 colon carcinoma cells)[1].
Dosage: 50 mg/kg
Administration: Orally administered, once daily, for 14 days
Result: Almost completely suppressed tumor growth, and the tumor concentration was high, with a tumor-to-plasma concentration ratio reflecting good distribution to the tumor.
Animal Model: Female BALB/c nude mice (inoculated with LoVo human colorectal xenograft)[1].
Dosage: 25 mg/kg and 50 mg/kg
Administration: Orally administered, once daily, for 19 days
Result: Significantly reduced tumor volume, and the effect was dose-dependent.
Animal Model: NOD/SCID IL2R gammanull mice (inoculated subcutaneously with  2×106 H929 myeloma cells)[2].
Dosage: 30 mg/kg
Administration: Orally administered, once daily, for up to 28 days
Result: Effectively inhibited tumor growth.
Clinical Trial
Molecular Weight

508.43

Formula

C22H20F4N6O4
CAS No.
SMILES

OC(C(F)(F)F)=O.FC(C=C1)=CC(C=C2)=C1N=C2CN[C@H]3[C@@]4([H])[C@]3([H])CN(C5=NC=C(C(NO)=O)C=N5)C4
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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Nanatinostat TFA 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:

Nanatinostat1256448-48-2CHR-3996CHR3996CHR 3996HDACApoptosisHistone deacetylasesHDAC1HDAC2HDAC3apoptosis myelomaadvanced solid tumours and colorectal cancerInhibitorinhibitorinhibit

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