GDC-0339
- CAS No.
- 1428569-85-0
- Chemical Name:
- GDC-0339
- Synonyms
- EOS-60554;GDC 0339,Pim,Pim kinases,inhibit,GDC0339,GDC-0339,Inhibitor;5-amino-N-(5-((4R,5R)-4-amino-5-fluoroazepan-1-yl)-1-methyl-1H-pyrazol-4-yl)-2-(2,6-difluorophenyl)thiazole-4-carboxamide;4-Thiazolecarboxamide, 5-amino-N-[5-[(4R,5R)-4-amino-5-fluorohexahydro-1H-azepin-1-yl]-1-methyl-1H-pyrazol-4-yl]-2-(2,6-difluorophenyl)-
- CBNumber:
- CB03035403
- Molecular Formula:
- C20H22F3N7OS
- Molecular Weight:
- 465.5
- MDL Number:
- MOL File:
- 1428569-85-0.mol
- MSDS File:
- SDS
- TDS File:
- TDS
| Density | 1.61±0.1 g/cm3(Predicted) |
|---|---|
| storage temp. | Store at -20°C |
| solubility | DMSO : ≥ 52 mg/mL (111.71 mM) |
| form | Solid |
| pka | 9.28±0.40(Predicted) |
| color | White to yellow |
| FDA UNII | 2PRJ7DX38T |
GDC-0339 price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Biosynth | DHC56985 | GDC-0339 | 1428569-85-0 | 1mg | $254.87 | 2026-06-04 | Buy |
| Biosynth | DHC56985 | GDC-0339 | 1428569-85-0 | 5mg | $828.3 | 2026-06-04 | Buy |
| Biosynth | DHC56985 | GDC-0339 | 1428569-85-0 | 10mg | $1325.3 | 2026-06-04 | Buy |
| Biosynth | DHC56985 | GDC-0339 | 1428569-85-0 | 25mg | $2485 | 2026-06-04 | Buy |
| Biosynth | DHC56985 | GDC-0339 | 1428569-85-0 | 50mg | $3976 | 2026-06-04 | Buy |
GDC-0339 Chemical Properties,Uses,Production
Uses
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[1][2].
in vivo
GDC-0339 (1-300 mg/kg; p.o; daily; for 21 days) is efficacious in RPMI8226 and MM.1S human multiple myeloma xenograft mouse models[2].
GDC-0339 has a half-life of t1/2=0.9 h[2].
| Animal Model: | Female C.B-17 SCID mice, RPMI8226 human multiple myeloma xenograft mouse model[2] |
| Dosage: | 1mg/kg, 10 mg/kg, 50 mg/kg, 100 mg/kg, 200 mg/kg, 300 mg/kg |
| Administration: | Oral administration; once daily; for 21 days |
| Result: | Showed dose-dependent tumor growth inhibition. |
IC 50
PIM1; PIM2; PIM3
References
[1] Takahashi RH, et al. CYP1A1-Mediated Intramolecular Rearrangement of Aminoazepane in GDC-0339. Drug Metab Dispos. 2017 Oct;45(10):1084-1092. DOI:10.1124/dmd.117.076786
[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. DOI:10.1021/acs.jmedchem.8b01857
GDC-0339 Preparation Products And Raw materials
Raw materials
Preparation Products
GDC-0339 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| BOC Sciences | 1-631-485-4226; 16314854226 | info@bocsci.com | United States | 9920 | 65 |
| Haoyuan Chemexpress Co., Ltd. | 021-58950125 | info@chemexpress.com | China | 7545 | 61 |
| MedChemexpress LLC | 021-58955995 | sales@medchemexpress.cn | United States | 4853 | 58 |
| Sichuan Wei Keqi Biological Technology Co., Ltd. | 028-81700200 18116577057 | 3003855609@qq.com | China | 7717 | 56 |
| SPIRO PHARMA | eric_feng1954@126.com | China | 9239 | 55 | |
| Shanghai EFE Biological Technology Co., Ltd. | 021-65675885 18964387627 | info@efebio.com | China | 9799 | 58 |
| Shanghai YuanYe Biotechnology Co., Ltd. | 15026964105 | 2881489226@qq.com | China | 89667 | 60 |
| Jinan elephant international trading co., LTD | 13006575422@163.com | China | 6347 | 58 | |
| Kaixin Chemical (Hong Kong) Limited | 010-88886666-01 13112345678 | loyson@qq.com | China | 589 | 55 |
| Musechem | +1-800-259-7612 | info@musechem.com | United States | 4648 | 60 |
