GNE-955

Alias: GNE-955; GNE 955; GNE955.
Cat No.:V4558 Purity: ≥98%
GNE-955 is a novel, potent and orally bioavailable panPim kinaseinhibitor withKis of 0.018, 0.11, 0.08 nM for Pim1, Pim2, Pim3, respectively.
GNE-955 Chemical Structure CAS No.: 1527523-39-2
Product category: New7
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

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.

Biological Activity I Assay Protocols (From Reference)
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]
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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C22H24N8O
Molecular Weight
416.4790
CAS #
1527523-39-2
SMILES
CC1=NC(C2=NC=C(C=NN3C4=CC=C(OC)C(N5CCC[C@H](N)C5)=C4)C3=C2)=CN=C1
InChi Key
ASRHSBIEFUFSJR-KRWDZBQOSA-N
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
Chemical Name
(S)-1-(2-methoxy-5-(6-(6-methylpyrazin-2-yl)-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl)piperidin-3-amine
Synonyms
GNE-955; GNE 955; GNE955.
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)
Solubility Data
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.

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