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TFMB-(R)-2-HG

Cat No.:V16204 Purity: ≥98%
TFMB-(R)-2-HG is cell membrane-permeable/penetrable (R)-2-HG, a carcinogen of acute myeloid leukemia (AML).
TFMB-(R)-2-HG
TFMB-(R)-2-HG Chemical Structure CAS No.: 1445700-01-5
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
10mg
50mg
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Other Forms of TFMB-(R)-2-HG:

  • TFMB-(S)-2-HG
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
TFMB-(R)-2-HG is cell membrane-permeable/penetrable (R)-2-HG, a carcinogen of acute myeloid leukemia (AML). TFMB-(R)-2-HG impairs SCF ER-Hoxb8 cell differentiation in response to estrogen withdrawal.
TFMB-(R)-2-HG (CAS 1445700-01-5) is a research compound that is a derivative or analog of (R)-2-hydroxyglutarate ((R)-2-HG). (R)-2-HG is an oncometabolite that accumulates in certain cancers due to mutations in isocitrate dehydrogenase (IDH) enzymes. TFMB-(R)-2-HG is used as a tool to study the role of (R)-2-HG in cancer metabolism and epigenetics.
Biological Activity I Assay Protocols (From Reference)
Targets
TFMB-(R)-2-HG targets the same pathways as (R)-2-hydroxyglutarate, including inhibition of α-ketoglutarate-dependent dioxygenases such as histone demethylases and DNA demethylases (TET enzymes). By mimicking (R)-2-HG, the compound modulates epigenetic regulation and cellular metabolism. The specific target and mechanism are described in the primary literature.
ln Vitro
In vitro activity of TFMB-(R)-2-HG is characterized by its effects on α-ketoglutarate-dependent dioxygenases and cellular metabolism. The compound's potency in inhibiting histone demethylases and TET enzymes is assessed in biochemical assays. Detailed in vitro activity data are available in the primary research literature.
ln Vivo
In vivo activity of TFMB-(R)-2-HG is evaluated in animal models of cancer and other diseases involving (R)-2-HG accumulation. The compound's effects on tumor growth, epigenetic regulation, and metabolic pathways are assessed. Detailed in vivo efficacy data are available in the primary research literature.
Enzyme Assay
In vitro enzyme assays for TFMB-(R)-2-HG measure its inhibition of α-ketoglutarate-dependent dioxygenases, including histone demethylases (e.g., KDM4, KDM5) and TET enzymes. The enzyme is incubated with its substrate and α-ketoglutarate in the presence of varying concentrations of the compound. Enzyme activity is measured by detecting demethylation or oxidation products. Detailed assay protocols are described in the primary literature.
Cell Assay
In vitro cell-based assays for TFMB-(R)-2-HG assess its effects on cellular metabolism, epigenetics, and gene expression. Cells are treated with the compound, and effects on histone methylation, DNA methylation, and gene expression are measured by Western blotting, LC-MS/MS, or RNA sequencing. Cell viability and proliferation are also assessed. Detailed cell-based assay protocols are described in the primary literature.
Animal Protocol
In vivo animal models for TFMB-(R)-2-HG include mouse models of IDH-mutant cancers. The compound is administered to tumor-bearing animals, and its effects on tumor growth, epigenetic markers, and survival are evaluated. Pharmacodynamic studies measure target engagement and pathway modulation. Detailed in vivo protocols are described in the primary literature.
ADME/Pharmacokinetics
Pharmacokinetic properties of TFMB-(R)-2-HG are described in the primary research literature. As a small-molecule analog of (R)-2-HG, its absorption, distribution, metabolism, and excretion are characterized in preclinical studies. Researchers should consult the relevant publications for detailed pharmacokinetic information.
Toxicity/Toxicokinetics
Toxicity data for TFMB-(R)-2-HG are available from preclinical safety studies. As a research compound, its safety profile is evaluated in standard toxicology studies. Researchers should consult the relevant publications for detailed toxicity information.
Additional Infomation
TFMB-(R)-2-HG (CAS 1445700-01-5) is a research compound used to study the role of (R)-2-hydroxyglutarate in cancer metabolism and epigenetics. The compound is intended for research use only and is not approved for clinical use. Detailed information on its chemical properties, biological activities, and research applications is available in the primary literature.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C13H11F3O4
Molecular Weight
288.22
Exact Mass
288.06
CAS #
1445700-01-5
Related CAS #
TFMB-(S)-2-HG;1445703-64-9
PubChem CID
91885414
Appearance
White to off-white solid powder
Density
1.4±0.1 g/cm3
Boiling Point
376.3±42.0 °C at 760 mmHg
Flash Point
175.2±22.8 °C
Vapour Pressure
0.0±0.9 mmHg at 25°C
Index of Refraction
1.494
LogP
1.14
Hydrogen Bond Donor Count
0
Hydrogen Bond Acceptor Count
7
Rotatable Bond Count
4
Heavy Atom Count
20
Complexity
380
Defined Atom Stereocenter Count
1
SMILES
O1C(=O)CC[C@@H]1C(OCC1=CC=CC(C(F)(F)F)=C1)=O
InChi Key
UXTLNUGKDZMPTC-SNVBAGLBSA-N
InChi Code
InChI=1S/C13H11F3O4/c14-13(15,16)9-3-1-2-8(6-9)7-19-12(18)10-4-5-11(17)20-10/h1-3,6,10H,4-5,7H2/t10-/m1/s1
Chemical Name
[3-(trifluoromethyl)phenyl]methyl (2R)-5-oxooxolane-2-carboxylate
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ≥ 250 mg/mL (~867.39 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.22 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.08 mg/mL (7.22 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.08 mg/mL (7.22 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.4696 mL 17.3479 mL 34.6957 mL
5 mM 0.6939 mL 3.4696 mL 6.9391 mL
10 mM 0.3470 mL 1.7348 mL 3.4696 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
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  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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