| Identification | Back Directory | [Name]
GDC-0339 | [CAS]
1428569-85-0 | [Synonyms]
EOS-60554
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)- | [Molecular Formula]
C20H22F3N7OS | [MOL File]
1428569-85-0.mol | [Molecular Weight]
465.5 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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 | [storage]
Store at -20°C | [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 |
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| Company Name: |
SPIRO PHARMA
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| Telephone: |
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| Website: |
www.spiropharma.com.cn |
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