WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406342
Description: GNE-900 is an ATP-competitive, selective, and orally bioavailable ChK1 inhibitor. In combination with chemotherapeutic agents, GNE-900 sustains ATR/ATM signaling, enhances DNA damage, and induces apoptotic cell death. GNE-900 has little single-agent activity in the absence of chemotherapy and does not grossly potentiate the cytotoxicity of gemcitabine in normal bone marrow cells. In vivo scheduling studies show that optimal administration of the ChK1 inhibitor requires a defined lag between gemcitabine and GNE-900 administration. (Mol Cancer Ther; 12(10); 1968-80).
MedKoo Cat#: 406342
Chemical Formula: C23H21N5
Exact Mass: 367.1797
Molecular Weight: 367.45
Elemental Analysis: C, 75.18; H, 5.76; N, 19.06
Synonym: GNE900; GNE-900; GNE 900.
IUPAC/Chemical Name: 3-(4-(piperidin-1-ylmethyl)phenyl)-9H-pyrrolo[2,3-b:5,4-c']dipyridine-6-carbonitrile
InChi Key: PPYHOOZGDDPLKM-UHFFFAOYSA-N
InChi Code: InChI=1S/C23H21N5/c24-12-19-11-20-21-10-18(13-26-23(21)27-22(20)14-25-19)17-6-4-16(5-7-17)15-28-8-2-1-3-9-28/h4-7,10-11,13-14H,1-3,8-9,15H2,(H,26,27)
SMILES Code: N#CC1=NC=C2C(C3=CC(C4=CC=C(CN5CCCCC5)C=C4)=CN=C3N2)=C1
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs
Storage Condition: 0 Â– 4 C for short term (weeks to 1 month) or -20 C for long terms (months to years).
Solubility: Soluble in DMSO, not soluble in water.
Shelf Life: >2 years if stored properly.
Drug Formulation: Stock solution storage:
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 367.45 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: Xiao Y, Ramiscal J, Kowanetz K, Del Nagro C, Malek S, Evangelista M, Blackwood E, Jackson PK, O'Brien T. Identification of Preferred Chemotherapeutics for Combining with a CHK1 Inhibitor. Mol Cancer Ther. 2013 Nov;12(11):2285-95. doi: 10.1158/1535-7163.MCT-13-0404. Epub 2013 Sep 13. PubMed PMID: 24038068.
2: Blackwood E, Epler J, Yen I, Flagella M, O'Brien T, Evangelista M, Schmidt S, Xiao Y, Choi J, Kowanetz K, Ramiscal J, Wong K, Jakubiak D, Yee S, Cain G, Gazzard L, Williams K, Halladay J, Jackson PK, Malek S. Combination Drug Scheduling Defines a "Window of Opportunity" for Chemopotentiation of Gemcitabine by an Orally Bioavailable, Selective ChK1 Inhibitor, GNE-900. Mol Cancer Ther. 2013 Oct;12(10):1968-80. doi: 10.1158/1535-7163.MCT-12-1218. Epub 2013 Jul 19. PubMed PMID: 23873850.