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Purity: ≥98%
GDC-0339 (GDC0339) is a novel, orally bioavailable, potent and selective small molecule pan-Pim kinase inhibitor with anticancer activity. It inhibits PIM with IC50 of 43.6 nM for BaF3 PIM1. GDC-0339 was discovered as a potential treatment of multiple myeloma.
| ln Vitro |
MM.1S cells exhibit cytostatic effects of GDC-0339, with an IC50 of 0.1 μM [2]. Following GDC-0339 therapy, a number of Pim downstream signaling events that were in line with Pim kinase inhibition were observed [2].
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| ln Vivo |
GDC-0339 (1-300 mg/kg; oral; daily; 21 days) shows efficacy in human multiple myeloma xenograft mouse models RPMI8226 and MM.1S [2]. GDC-0339 has a half-life of t1/2=0.9 h[2].
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| Cell Assay |
Cell viability assay [2]
Cell Types: MM.1S Cell Tested Concentrations: Incubation Duration: 3 days Experimental Results: Cell viability was inhibited. Western Blot Analysis[2] Cell Types: MM.1S Cell Tested Concentrations: 0.01 μM, 0.03 μM, 0.09 μM, 0.27 μM, 0.83 μM, 2.5 μM Incubation Duration: 4 hrs (hours) Experimental Results: Induction of a series of Pim downstream signaling events consistent with inhibition Pim kinase. |
| Animal Protocol |
Animal/Disease Models: Female CB-17 SCID mouse, RPMI8226 human multiple myeloma xenograft mouse model [2]
Doses: 1mg/kg, 10mg/kg, 50mg/kg, 100mg/kg, 200mg/kg, 300mg/kg Doses: po (po (oral gavage)) one time/day; for 21 days. Experimental Results: demonstrated dose-dependent tumor growth inhibition. |
| References |
[1]. Takahashi RH, et al. CYP1A1-Mediated Intramolecular Rearrangement of Aminoazepane in GDC-0339. Drug Metab Dispos. 2017 Oct;45(10):1084-1092.
[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. |
| Molecular Formula |
C20H22F3N7OS
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| Molecular Weight |
465.4952
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| CAS # |
1428569-85-0
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| SMILES |
O=C(C1=C(N)SC(C2=C(F)C=CC=C2F)=N1)NC3=C(N4CC[C@@H](N)[C@H](F)CC4)N(C)N=C3
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| InChi Key |
NHXVGMQFCYBLTL-ZWNOBZJWSA-N
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| InChi Code |
InChI=1S/C20H22F3N7OS/c1-29-20(30-7-5-10(21)13(24)6-8-30)14(9-26-29)27-18(31)16-17(25)32-19(28-16)15-11(22)3-2-4-12(15)23/h2-4,9-10,13H,5-8,24-25H2,1H3,(H,27,31)/t10-,13-/m1/s1
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| Chemical Name |
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
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| Synonyms |
GDC0339; GDC 0339; GDC-0339
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 52 mg/mL (~111.71 mM)
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1482 mL | 10.7411 mL | 21.4823 mL | |
| 5 mM | 0.4296 mL | 2.1482 mL | 4.2965 mL | |
| 10 mM | 0.2148 mL | 1.0741 mL | 2.1482 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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