[CAS NO. 1168091-68-6] GDC-0623
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PRODUCTS SPECIFICATIONS [1168091-68-6]
Catalog
SLK-S7553
Brand
Selleck
CAS
1168091-68-6
DESCRIPTION [1168091-68-6]
Overview
| MDL | MFCD25976760 |
|---|---|
| Molecular Weight | 456.21 |
| Molecular Formula | C16H14FIN4O3 |
| SMILES | O=C(C1=C(NC2=CC=C(I)C=C2F)N3C(C=C1)=CN=C3)NOCCO |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1920 mL | 10.9599 mL | 21.9197 mL |
| 5 mM | 0.4384 mL | 2.1920 mL | 4.3839 mL |
| 10 mM | 0.2192 mL | 1.0960 mL | 2.1920 mL |
| 50 mM | 0.0438 mL | 0.2192 mL | 0.4384 mL |
Description
GDC-0623 (G-868) is a potent and ATP-uncompetitive inhibitor with of 0.13 nM. Phase 1.
Targets
| MEK1 [1] |
| 0.13 nM |
In vitro
In a panel of mutant cancer cell lines, GDC-0623 inhibits cellular proliferation with EC50 of 4 nM, 53 nM, 11 nM, 18 nM and 94 nM for A375 (BRAFV600E), HCT116 (KRASG13D), COLO 205 (V600E), HT-29 (V600E), and HCT116 (G13D) cells, respectively. In isogenic KRAS HCT116 and mutant KRAS SW620 colon cells, GDC-0623 upregulates BIM via its loss of phosphorylation at Ser69. GDC-0623 plus ABT-263 induces a synergistic cell apoptosis.
In vivo
In vivo, GDC-0623 (40 mg/kg, p.o.) causes potent tumor growth inhibition (TGI) in mouse MiaPaCa-2 (120%), A375 (102%) and HCT116 (115%) xenografts.
References
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