G007-LK
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- CAS-Nr.
- 1380672-07-0
- Englisch Name:
- G007-LK
- Synonyma:
- G007-LK;CS-1659;G007 LK;G007LK;G007-LK;G007 LK;G007LK;G007-LK, 10 mM in DMSO;Tankyrase 1/2 Inhibitor VI, G007-LK;Tankyrase 1/2 Inhibitor VI, G007-LK - Calbiochem;G007LK,Inhibitor,poly ADP ribose polymerase,G-007-LK,G007 LK,PARP,inhibit,G007-LK;(E)-4-(5-(2-(4-(2-chlorophenyl)-5-(5-(methylsulfonyl)pyridin-2-yl)-4H-1,2,4-triazol-3-yl)vinyl)-1,3,4-oxadiazol-2-yl)benzonitrile;4-[5-[(1E)-2-[4-(2-Chlorophenyl)-5-[5-(methylsulfonyl)-2-pyridinyl]-4H-1,2,4-triazol-3-yl]ethenyl]-1,3,4-oxadiazol-2-yl]benzonitrile
- CBNumber:
- CB32707548
- Summenformel:
- C25H16ClN7O3S
- Molgewicht:
- 529.96
- MOL-Datei:
- 1380672-07-0.mol
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G007-LK Eigenschaften
- Siedepunkt:
- 817.3±75.0 °C(Predicted)
- Dichte
- 1.47±0.1 g/cm3(Predicted)
- storage temp.
- +2C to +8C
- L?slichkeit
- ≥26.5 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
- Aggregatzustand
- White powder
- pka
- -1.68±0.10(Predicted)
- Farbe
- Off-white to yellow
- InChI
- 1S/C25H16ClN7O3S/c1-37(34,35)18-10-11-20(28-15-18)24-31-29-22(33(24)21-5-3-2-4-19(21)26)12-13-23-30-32-25(36-23)17-8-6-16(14-27)7-9-17/h2-13,15H,1H3/b13-12+
- InChIKey
- HIWVLHPKZNBSBE-OUKQBFOZSA-N
- SMILES
- [S](=O)(=O)(C)c1cnc(cc1)c2[n](c(nn2)\C=C\c4nnc([o]4)c5ccc(cc5)C#N)c3c(cccc3)Cl
Sicherheit
- Risiko- und Sicherheitserkl?rung
- Gefahreninformationscode (GHS)
| WGK Germany |
WGK 2 |
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| Speicherklasse |
11 - Combustible Solids |
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| Bildanzeige (GHS) |
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| Alarmwort |
Achtung
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| Gefahrenhinweise |
| Code |
Gefahrenhinweise |
Gefahrenklasse |
Abteilung |
Alarmwort |
Symbol |
P-Code |
| H301 |
Giftig bei Verschlucken. |
Akute Toxizit?t oral |
Kategorie 3 |
Achtung |
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P264, P270, P301+P310, P321, P330,P405, P501 |
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| Sicherheit |
| P301+P310 |
BEI VERSCHLUCKEN: Sofort GIFTINFORMATIONSZENTRUM/Arzt/... (geeignete Stelle für medizinische Notfallversorgung vom Hersteller/Lieferanten anzugeben) anrufen. |
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G007-LK Chemische Eigenschaften,Einsatz,Produktion Methoden
Allgemeine Beschreibung
A cell-permeable, triazolyl-vinyl-oxadiazole compound that targets adenosine site of the NAD
+ pocket in the TNKS PARP domain and acts as a potent and highly selective tankyrase inhibitor (IC
50 = 33 and 26 nM, respectively, against TNKS1/PARP5a/ARTD5 and TNKS2/PARP5b/ARTD6 in auto-PARsylation assays), effectively inhibiting murine Wnt3a-induced reporter activity in human HEK293 and murine 10T1/2 cultures (IC
max ~300 and 600 nM, respectively). Shown to display little or no inhibitory potency (IC
50 >10 μM) toward 7 other PARP enzymes (PARP1, 2, 3, 6, 7,10,11), 90 kinases, 16 phosphatases, and 75 GPCRs (IC
50 >10 μM). Shown to inhibit two CRC lines, COLO-320DM & SW403, colony formation
in vitro (200 nM) and tumor expansion in mice
in vivo (20 mg/kg via daily i.p.), although G007-LK toxicity is observed at higher dosages (≥30 mg/kg/12 h or 60 mg/kg/d via i.p.).
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Biochem/physiol Actions
Cell permeable: yes
G007-LK Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
G007-LK Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 112)Lieferanten
- G007-LK
- (E)-4-(5-(2-(4-(2-chlorophenyl)-5-(5-(methylsulfonyl)pyridin-2-yl)-4H-1,2,4-triazol-3-yl)vinyl)-1,3,4-oxadiazol-2-yl)benzonitrile
- 4-[5-[(1E)-2-[4-(2-Chlorophenyl)-5-[5-(methylsulfonyl)-2-pyridinyl]-4H-1,2,4-triazol-3-yl]ethenyl]-1,3,4-oxadiazol-2-yl]benzonitrile
- Benzonitrile, 4-[5-[(1E)-2-[4-(2-chlorophenyl)-5-[5-(methylsulfonyl)-2-pyridinyl]-4H-1,2,4-triazol-3-yl]ethenyl]-1,3,4-oxadiazol-2-yl]-
- G007-LK;G007 LK;G007LK
- CS-1659
- Tankyrase 1/2 Inhibitor VI, G007-LK - Calbiochem
- G007 LK;G007LK
- G007LK,Inhibitor,poly ADP ribose polymerase,G-007-LK,G007 LK,PARP,inhibit,G007-LK
- G007-LK, 10 mM in DMSO
- Tankyrase 1/2 Inhibitor VI, G007-LK
- 1380672-07-0
- C25H16ClN7O3S
