2. Epigenetics Apoptosis
  3. Histone Methyltransferase Apoptosis
  4. PF-06939999

PF-06939999  (Synonyms: PRMT5-IN-3)

Cat. No.: HY-131493 Purity: 99.84%
Data Sheet
SDS
COA
Handling Instructions Technical Support

Solubility

In Vivo Dissolution Calculator

PF-06939999 (PRMT5-IN-3) is a SAM-competitive, orally active PRMT5 inhibitor that inhibits the expression of SDMA protein (IC50 in A427 is 1.1 nM). PF-06939999 exhibits antitumor effect.

For research use only. We do not sell to patients.

PF-06939999 Chemical Structure

PF-06939999 Chemical Structure

CAS No. : 2159123-14-3

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1 mg USD 242 In-stock
5 mg USD 580 In-stock
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25 mg USD 1854 In-stock
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Based on 1 publication(s) in Google Scholar

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 ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PF-06939999 (PRMT5-IN-3) is a SAM-competitive, orally active PRMT5 inhibitor that inhibits the expression of SDMA protein (IC50 in A427 is 1.1 nM). PF-06939999 exhibits antitumor effect[1][2].

IC50 & Target

PRMT5

 

In Vitro

PF-06939999 competitively binds to the cofactor binding site of PRMT5， interferes with its splicing process, leads to splicing changes such as exon skipping and intron retention, thereby affecting cellular functions[2].
PF-06939999 (0.1 nM-10 μM, 7 days) inhibits the proliferation of NSCLC cell A427, NCI-H441, NCI-H1975 and A549, arrests the cell cycle of A427 at G1 phase, arrests the cell cycle of NCI-H1975 at G2/M phase, induces apoptosis in A427 cell[2].
PF-06939999 (30 nM, 10 days) causes cell morphological changes and positive β-galactosidase staining, inducing cell senescence in A549 cell[2].

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

Cell Proliferation Assay[2]

Cell Line: A427, NCI-H441, NCI-H1975 and A549
Concentration: 0.1 nM-1 μM
Incubation Time: 5 days
Result: Inhibited cell proliferation.

Cell Cycle Analysis[2]

Cell Line: A427 and NCI-H1975
Concentration: 0.3-300 nM
Incubation Time: 5 days
Result: Arrested the cell cycle of A427 at G1 phase, arrested the cell cycle of NCI-H1975 at G2/M phase.
In Vivo

PF-06939999 (3-30 mg/kg, po, once a day for 36-44 days) exhibits antitumor effect in mouse A427 or NCI-H441 xenograft models[2].

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

Animal Model: Mouse A427 or NCI-H441 xenograft models[2]
Dosage: 3-30 mg/kg
Administration: po, once a day for 36-44 days
Result: Inhibited tumor growth.
Clinical Trial
Molecular Weight

448.44

Formula

C22H23F3N4O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O[C@@H]1[C@H](O)[C@@H](OC2=CC(C(F)F)=C(F)C3=C2CNCC3)C[C@H]1N4C=CC5=C(C)N=CN=C54
Shipping

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

H2O : 100 mg/mL (223.00 mM; Need ultrasonic)

DMSO : 100 mg/mL (223.00 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 2.2300 mL 11.1498 mL 22.2995 mL
5 mM 0.4460 mL 2.2300 mL 4.4599 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • 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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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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C2

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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.
Purity & Documentation

Purity: 99.84%

Data Sheet (278 KB) SDS (251 KB)

COA (256 KB) HNMR (226 KB) LCMS (95 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
H2O / DMSO 1 mM 2.2300 mL 11.1498 mL 22.2995 mL 55.7488 mL
5 mM 0.4460 mL 2.2300 mL 4.4599 mL 11.1498 mL
10 mM 0.2230 mL 1.1150 mL 2.2300 mL 5.5749 mL
15 mM 0.1487 mL 0.7433 mL 1.4866 mL 3.7166 mL
20 mM 0.1115 mL 0.5575 mL 1.1150 mL 2.7874 mL
25 mM 0.0892 mL 0.4460 mL 0.8920 mL 2.2300 mL
30 mM 0.0743 mL 0.3717 mL 0.7433 mL 1.8583 mL
40 mM 0.0557 mL 0.2787 mL 0.5575 mL 1.3937 mL
50 mM 0.0446 mL 0.2230 mL 0.4460 mL 1.1150 mL
60 mM 0.0372 mL 0.1858 mL 0.3717 mL 0.9291 mL
80 mM 0.0279 mL 0.1394 mL 0.2787 mL 0.6969 mL
100 mM 0.0223 mL 0.1115 mL 0.2230 mL 0.5575 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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PF-06939999 Related Classifications

Keywords:

PF-069399992159123-14-3PRMT5-IN-3PF06939999PF 06939999Histone MethyltransferaseApoptosisA427NCI-H441NCI-H1975A549orally activeInhibitorinhibitorinhibit

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