PRMT5-IN-35
Based on 1 Customer Validation
PRMT5-IN-35 (Compound 87) is a potent, selective and orally active PRMT5 inhibitor with an IC50 value of 1 nM. PRMT5-IN-35 can be used in cancer research.
For research use only. We do not sell to patients.
- Purity : 99.30%
- CAS No.: 1989620-03-2
- Formula: C17H17ClN4O4
- Molecular Weight:376.79
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Histone Methyltransferase Isoforms
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Biological Activity
Description
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
10.8 nM
Compound: 46
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Antiproliferation activity against human A-375 cells assessed as cell growth inhibition
Antiproliferation activity against human A-375 cells assessed as cell growth inhibition
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[PMID: 36274274] |
| A-375 | IC50 |
11 nM
Compound: 2
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Antiproliferative activity against human A375 cells measured after 7 days by cell titer glo-based luminescence assay
Antiproliferative activity against human A375 cells measured after 7 days by cell titer glo-based luminescence assay
|
[PMID: 30956011] |
| A549 | IC50 |
5 nM
Compound: 2
|
Antiproliferative activity against human A549 cells incubated for 7 days with compound replacement on day 4 by cell titer glo-based luminescence assay
Antiproliferative activity against human A549 cells incubated for 7 days with compound replacement on day 4 by cell titer glo-based luminescence assay
|
[PMID: 30956011] |
| Sf21 | IC50 |
1 nM
Compound: 2
|
Inhibition of full length N-terminal FLAG-tagged PRMT5 (unknown origin)/MEP50 (unknown origin) expressed in baculovirus infected Sf21 insect cells using H4(1-21) peptide SGRGKGGKGLGKGGAKRHRKV as substrate measured after 25 minutes in the presence of [3H]S
Inhibition of full length N-terminal FLAG-tagged PRMT5 (unknown origin)/MEP50 (unknown origin) expressed in baculovirus infected Sf21 insect cells using H4(1-21) peptide SGRGKGGKGLGKGGAKRHRKV as substrate measured after 25 minutes in the presence of [3H]S
|
[PMID: 30956011] |
| Sf9 | IC50 |
4.3 nM
Compound: 2
|
Inhibition of recombinant human N-terminal FLAG-tagged PRMT5 (1 to 637 residue) /full length human N-terminal His tagged MEP50 expressed in baculovirus infected Sf9 insect cells assessed as reduction in methyl transfer from [3H]-SAM to biotinylated histon
Inhibition of recombinant human N-terminal FLAG-tagged PRMT5 (1 to 637 residue) /full length human N-terminal His tagged MEP50 expressed in baculovirus infected Sf9 insect cells assessed as reduction in methyl transfer from [3H]-SAM to biotinylated histon
|
[PMID: 30956011] |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1989620-03-2
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Appearance Solid
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Molecular Weight 376.79
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Formula C17H17ClN4O4
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Color White to off-white
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SMILES
O[C@H]1[C@@H](O)[C@H](N2C3=NC=NC(N)=C3C=C2)O[C@@H]1[C@H](O)C4=CC=C(Cl)C=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
In Vitro:
DMSO : 125 mg/mL (331.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
Purity & Documentation
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Data Sheet (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6540 mL | 13.2700 mL | 26.5400 mL | 66.3500 mL |
| 5 mM | 0.5308 mL | 2.6540 mL | 5.3080 mL | 13.2700 mL | |
| 10 mM | 0.2654 mL | 1.3270 mL | 2.6540 mL | 6.6350 mL | |
| 15 mM | 0.1769 mL | 0.8847 mL | 1.7693 mL | 4.4233 mL | |
| 20 mM | 0.1327 mL | 0.6635 mL | 1.3270 mL | 3.3175 mL | |
| 25 mM | 0.1062 mL | 0.5308 mL | 1.0616 mL | 2.6540 mL | |
| 30 mM | 0.0885 mL | 0.4423 mL | 0.8847 mL | 2.2117 mL | |
| 40 mM | 0.0663 mL | 0.3317 mL | 0.6635 mL | 1.6587 mL | |
| 50 mM | 0.0531 mL | 0.2654 mL | 0.5308 mL | 1.3270 mL | |
| 60 mM | 0.0442 mL | 0.2212 mL | 0.4423 mL | 1.1058 mL | |
| 80 mM | 0.0332 mL | 0.1659 mL | 0.3317 mL | 0.8294 mL | |
| 100 mM | 0.0265 mL | 0.1327 mL | 0.2654 mL | 0.6635 mL |