Size | Price | |
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10mg | ||
25mg | ||
50mg | ||
100mg | ||
250mg |
Purity: ≥98%
GNE-955 is a novel, potent and orally bioavailable pan Pim kinase inhibitor with Kis of 0.018, 0.11, 0.08 nM for Pim1, Pim2, Pim3, respectively. Pim kinases have been identified as promising therapeutic targets for hematologic-oncology indications, including multiple myeloma and certain leukemia. GNE-955 was discovered bearing 5-azaindazole core with noncanonical hydrogen bonding to the hinge.
ln Vitro |
After 72 hours of treatment, GNE-955 has an IC50 value of 0.5 μM, which suppresses the growth of MM.1S cells [1]. With no impact on the overall amounts of BAD, S6, or 4EBP protein, GNE-955 (0.156-5 μM) suppresses the phosphorylation of BAD (s112), S6 (s235/236), S6 (s240/244), and 4EBP (s65). [1]
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References |
[1]. Wang X, et al. Discovery of 5-Azaindazole (GNE-955) as a Potent Pan-Pim Inhibitor with Optimized Bioavailability. J Med Chem. 2017 May 25;60(10):4458-4473.
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Molecular Formula |
C22H24N8O
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Molecular Weight |
416.4790
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CAS # |
1527523-39-2
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SMILES |
CC1=NC(C2=NC=C(C=NN3C4=CC=C(OC)C(N5CCC[C@H](N)C5)=C4)C3=C2)=CN=C1
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InChi Key |
ASRHSBIEFUFSJR-KRWDZBQOSA-N
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InChi Code |
InChI=1S/C23H25N7O/c1-15-10-25-13-20(28-15)19-9-21-16(11-26-19)12-27-30(21)18-5-6-23(31-2)22(8-18)29-7-3-4-17(24)14-29/h5-6,8-13,17H,3-4,7,14,24H2,1-2H3/t17-/m0/s1
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Chemical Name |
(S)-1-(2-methoxy-5-(6-(6-methylpyrazin-2-yl)-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl)piperidin-3-amine
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Synonyms |
GNE-955; GNE 955; GNE955.
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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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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4011 mL | 12.0054 mL | 24.0108 mL | |
5 mM | 0.4802 mL | 2.4011 mL | 4.8022 mL | |
10 mM | 0.2401 mL | 1.2005 mL | 2.4011 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.