GDC-0339
- Product Name
- 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
- Formula Weight
- 465.5
- MOL File
- 1428569-85-0.mol
GDC-0339 Property
- 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
N-Bromosuccinimide Price
- Product number
- CS-4775
- Product name
- GDC-0339
- Purity
- 99.96%
- Packaging
- 5mg
- Price
- $500
- Updated
- 2021/12/16
- Product number
- CS-4775
- Product name
- GDC-0339
- Purity
- 99.96%
- Packaging
- 10mg
- Price
- $800
- Updated
- 2021/12/16
- Product number
- CS-4775
- Product name
- GDC-0339
- Purity
- 99.96%
- Packaging
- 50mg
- Price
- $2600
- Updated
- 2021/12/16
- Product number
- CS-4775
- Product name
- GDC-0339
- Purity
- 99.96%
- Packaging
- 100mg
- Price
- $4500
- Updated
- 2021/12/16
GDC-0339 Chemical Properties,Usage,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
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