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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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G648750-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $166.90 | |
G648750-10mg | 10mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $291.90 | |
G648750-25mg | 25mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $616.90 | |
G648750-50mg | 50mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $1,083.90 |
Storage Temp | Store at -20°C |
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Shipped In | Ice chest + Ice pads |
Product Description | GNE-900 is a an ATP-competitive, selective, and orally active ChK1 inhibitor with IC 50 s of 0.0011, 1.5 µM for ChKl, ChK2 , respectively. GNE-900 abrogates the G2-M checkpoint, enhances DNA damage, and induces Apoptosis . gemcitabine ( HY-17026 ) and GNE-900 administration shows anti-tumor activity In Vitro GNE-900 (1 µM; 1-48 h) induces apoptosis with increases in the expression of cleaved PARP when combined with gemcitabine (50 nM) in HT-29 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Apoptosis AnalysisCell Line: HT-29 cells Concentration: 1 µM Incubation Time: 1-48 h Result: Inducesd apoptosis with increased the expression of cleaved PARP when combination with gemcitabine (50 nM). In Vivo GNE-900 (2.5-40 mg/kg; p.o.; once) decreases the tumor volume and increases DNA damage, γ-H2AX levels when combinated with gemcitabine (HY-17026) in rats . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Sprague-Dawley rats (HT-29 tumor xenografts) Dosage: 2.5-40 mg/kg (received a dose of gemcitabine 120 mg/kg) Administration: P.o.; once Result: Decreased the tumor volume and resulted in significant enhancement of DNA damage, increased γ-H2AX levels. IC50& Target:Chk1 0.0011 μM (IC 50 ) Chk2 1.5 μM (IC 50 ) |
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IUPAC Name | 12-[4-(piperidin-1-ylmethyl)phenyl]-5,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2(7),3,5,10,12-hexaene-4-carbonitrile |
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INCHI | 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) |
InChi Key | PPYHOOZGDDPLKM-UHFFFAOYSA-N |
Canonical SMILES | C1CCN(CC1)CC2=CC=C(C=C2)C3=CC4=C(NC5=C4C=C(N=C5)C#N)N=C3 |
Isomeric SMILES | C1CCN(CC1)CC2=CC=C(C=C2)C3=CC4=C(NC5=C4C=C(N=C5)C#N)N=C3 |
PubChem CID | 44545757 |
MeSH Entry Terms | 3-(4-(1-piperidinylmethyl)phenyl)-9H-pyrrolo(2,3-b-5,4-c')dipyridine-6-carbonitrile;GNE-900 |
Molecular Weight | 367.45 |
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