GDC-0339
Based on 2 publication(s) in Google Scholar
GDC-0339 is a potent, orally bioavailable and well tolerated pan-Pim kinase inhibitor, with Kis of 0.03 nM, 0.1 nM and 0.02 nM for Pim1, Pim2 and Pim3, respectively. GDC-0339 is discovered as a potential treatment of multiple myeloma.
For research use only. We do not sell to patients.
- Purity: 99.87%
- CAS No.: 1428569-85-0
- Formula: C20H22F3N7OS
- Molecular Weight:465.50
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) GDC-0339
More
Biological Activity
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PIM1 |
PIM2 |
PIM3 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
2.7 μM
Compound: 16; GDC-0339
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Inhibition of human ERG expressed in HEK293 cells after 5 mins by patch clamp assay
Inhibition of human ERG expressed in HEK293 cells after 5 mins by patch clamp assay
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[PMID: 30715878] |
| MM1.S | IC50 |
0.03 μM
Compound: 16; GDC-0339
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Antiproliferative activity against human MM1S cells after 72 hrs in presence of PI3K inhibitor GDC-0941 by CellTiter-Glo assay
Antiproliferative activity against human MM1S cells after 72 hrs in presence of PI3K inhibitor GDC-0941 by CellTiter-Glo assay
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[PMID: 30715878] |
| MM1.S | IC50 |
0.07 μM
Compound: 16; GDC-0339
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Antiproliferative activity against human MM1S cells after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human MM1S cells after 72 hrs by CellTiter-Glo assay
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[PMID: 30715878] |
GDC-0339 is cytostatic, with an IC50 of 0.1 μM for MM.1S cells[2].
GDC-0339 treatment reveals a constellation of Pim downstream signaling events consistent with inhibition of Pim kinases[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MM.1S cells
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Concentration:
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Incubation Time:3 days
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Result:Inhibited cell viability.
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Cell Line:MM.1S cells
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Concentration:0.01 μM, 0.03 μM, 0.09 μM,0.27 μM, 0.83 μM, 2.5 μM
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Incubation Time:4 hours
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Result:Induced a constellation of Pim downstream signaling events consistent with inhibition of Pim kinases.
GDC-0339 has a half-life of t1/2=0.9 h[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female C.B-17 SCID mice, RPMI8226 human multiple myeloma xenograft mouse model[2]
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Dosage:1mg/kg, 10 mg/kg, 50 mg/kg, 100 mg/kg, 200 mg/kg, 300 mg/kg
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Administration:Oral administration; once daily; for 21 days
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Result:Showed dose-dependent tumor growth inhibition.
Chemical Information
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CAS No. 1428569-85-0
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Appearance Solid
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Molecular Weight 465.50
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Formula C20H22F3N7OS
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Color White to yellow
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SMILES
FC1=CC=CC(F)=C1C2=NC(C(NC3=C(N4CC[C@@H](F)[C@H](N)CC4)N(C)N=C3)=O)=C(N)S2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Cell Chem Biol
Synergistic PIM kinase and proteasome inhibition as a therapeutic strategy for MYC-overexpressing triple-negative breast cancer. [Abstract]2022 Mar 17;29(3):358-372.e5. PMID: 34525344 -
Commun Med (Lond)
S100A8/A9 predicts response to PIM kinase and PD-1/PD-L1 inhibition in triple-negative breast cancer mouse models. [Abstract]2024 Feb 20;4(1):22. PMID: 38378783
Solvent & Solubility
DMSO : ≥ 52 mg/mL (111.71 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (281 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
[1]. Takahashi RH, et al. CYP1A1-Mediated Intramolecular Rearrangement of Aminoazepane in GDC-0339. Drug Metab Dispos. 2017 Oct;45(10):1084-1092. [Content Brief]
[2]. Wang X, et al. Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma. J Med Chem. 2019 Feb 28;62(4):2140-2153. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1482 mL | 10.7411 mL | 21.4823 mL | 53.7057 mL |
| 5 mM | 0.4296 mL | 2.1482 mL | 4.2965 mL | 10.7411 mL | |
| 10 mM | 0.2148 mL | 1.0741 mL | 2.1482 mL | 5.3706 mL | |
| 15 mM | 0.1432 mL | 0.7161 mL | 1.4322 mL | 3.5804 mL | |
| 20 mM | 0.1074 mL | 0.5371 mL | 1.0741 mL | 2.6853 mL | |
| 25 mM | 0.0859 mL | 0.4296 mL | 0.8593 mL | 2.1482 mL | |
| 30 mM | 0.0716 mL | 0.3580 mL | 0.7161 mL | 1.7902 mL | |
| 40 mM | 0.0537 mL | 0.2685 mL | 0.5371 mL | 1.3426 mL | |
| 50 mM | 0.0430 mL | 0.2148 mL | 0.4296 mL | 1.0741 mL | |
| 60 mM | 0.0358 mL | 0.1790 mL | 0.3580 mL | 0.8951 mL | |
| 80 mM | 0.0269 mL | 0.1343 mL | 0.2685 mL | 0.6713 mL | |
| 100 mM | 0.0215 mL | 0.1074 mL | 0.2148 mL | 0.5371 mL |
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