2. Epigenetics
  3. Epigenetic Reader Domain Histone Methyltransferase
  4. PF-06821497

PF-06821497 (compound 23a) is a potent, selective and orally active Enhancer of Zeste Homolog 2 (EZH2) inhibitor, with a Ki value <0.1 nM against mutant Y641N EZH2. Exhibits robust tumor growth inhibition.

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PF-06821497 Chemical Structure

PF-06821497 Chemical Structure

CAS No. : 1844849-10-0

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5 mg USD 290 In-stock
10 mg USD 450 In-stock
25 mg USD 680 In-stock
50 mg USD 950 In-stock
100 mg USD 1250 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

PF-06821497 Related Antibodies

Top Publications Citing Use of Products

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PF-06821497 (compound 23a) is a potent, selective and orally active Enhancer of Zeste Homolog 2 (EZH2) inhibitor, with a Ki value <0.1 nM against mutant Y641N EZH2. Exhibits robust tumor growth inhibition[1].

IC50 & Target

Ki: <0.1 nM (Y641N EZH2)[1].
In Vivo

PF-06821497 (compound 23a: 100 mg/kg, PO twice daily for 31 days) treatment results in significant inhibition of tumor growth, and the the tumor regressition effect can be sustained for another 40 days after the terminal administration[1].
PF-06821497 with the dose of 300 mg/kg has minimal impact on animal body weights[1].

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

Animal Model: Mice bearing Karpas-422 DLBCL tumor xenografts (which contain the Y641N EZH2 mutation)[1].
Dosage: 100 mg/kg and 300 mg/kg.
Administration: PO twice daily for 31 days.
Result: 100 mg/kg dose resulted in significant inhibition of tumor growth and 300 mg/kg dose minimal effected animal body weights.
Molecular Weight

467.34

Formula

C22H24Cl2N2O5
CAS No.
Appearance

Solid

SMILES

O=C1N(CC2=C(OC)C=C(C)NC2=O)CCC3=C1C(Cl)=C([C@H](OC)C4COC4)C=C3Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (213.98 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1398 mL 10.6988 mL 21.3977 mL
5 mM 0.4280 mL 2.1398 mL 4.2795 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.35 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.35 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.37% ee.: 100%

COA (251 KB) HNMR (429 KB) RP-HPLC (252 KB) NP-HPLC (252 KB) LCMS (88 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1398 mL 10.6988 mL 21.3977 mL 53.4942 mL
5 mM 0.4280 mL 2.1398 mL 4.2795 mL 10.6988 mL
10 mM 0.2140 mL 1.0699 mL 2.1398 mL 5.3494 mL
15 mM 0.1427 mL 0.7133 mL 1.4265 mL 3.5663 mL
20 mM 0.1070 mL 0.5349 mL 1.0699 mL 2.6747 mL
25 mM 0.0856 mL 0.4280 mL 0.8559 mL 2.1398 mL
30 mM 0.0713 mL 0.3566 mL 0.7133 mL 1.7831 mL
40 mM 0.0535 mL 0.2675 mL 0.5349 mL 1.3374 mL
50 mM 0.0428 mL 0.2140 mL 0.4280 mL 1.0699 mL
60 mM 0.0357 mL 0.1783 mL 0.3566 mL 0.8916 mL
80 mM 0.0267 mL 0.1337 mL 0.2675 mL 0.6687 mL
100 mM 0.0214 mL 0.1070 mL 0.2140 mL 0.5349 mL
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PF-06821497 Related Classifications

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:

PF-068214971844849-10-0PF06821497PF 06821497Epigenetic Reader DomainHistone MethyltransferaseInhibitorinhibitorinhibit

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