ChemicalBook > CAS DataBase List > GDC-0339

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
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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
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene
Product number
CS-4775
Product name
GDC-0339
Purity
99.96%
Packaging
5mg
Price
$500
Updated
2021/12/16
ChemScene
Product number
CS-4775
Product name
GDC-0339
Purity
99.96%
Packaging
10mg
Price
$800
Updated
2021/12/16
ChemScene
Product number
CS-4775
Product name
GDC-0339
Purity
99.96%
Packaging
50mg
Price
$2600
Updated
2021/12/16
ChemScene
Product number
CS-4775
Product name
GDC-0339
Purity
99.96%
Packaging
100mg
Price
$4500
Updated
2021/12/16
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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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GDC-0339 Suppliers

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1428569-85-0, GDC-0339Related Search:


  • 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
  • EOS-60554
  • 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)-
  • GDC 0339,Pim,Pim kinases,inhibit,GDC0339,GDC-0339,Inhibitor
  • 1428569-85-0
  • C20H22F3N7OS