INCB159020
INCB159020 is an orally active KRASG12D inhibitor with equivalent binding potency for the active GTP-bound and inactive GDP-bound forms of KRASG12D. INCB159020 can be used in the research of KRAS-driven cancers.
Para uso exclusivo en investigación. No vendemos a pacientes.
- No. CAS: 2923669-20-7
- Fòrmula: C37H35ClFN7O2
- Peso molecular:664.17
-
Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
- Pureza y Documentación
- Referencias
-
Help & FAQs
Actividad biológica
|
KRas G12D |
INCB159020 (compound 23) exhibits comparable binding potency towards active GTP-bound and inactive GDP-bound KRASG12D, with a Kd of 2.4 nM for the GDP-bound form and 2.8 nM for the GTP-bound form[1].
INCB159020 inhibits the exchange activity of KRASG12D with an IC50 of 4.4 nM; it also inhibits ERK phosphorylation in the presence of human whole blood with an IC50 of 331 nM[1].
INCB159020 inhibits hERG channels with an IC50 of 11.2 μM, and exhibits a Caco-2 permeability of 3.6 × 10-6 cm/s[1].
INCB159020 exerts selective inhibitory effects on CYP3A4 and CYP2D6, with IC50 values of 17 μM and 7.2 μM, respectively[1].
INCB159020 inhibits ERK phosphorylation in KRASG12D-dependent HPAFII cells with an IC50 of 33 nM, and reduces the viability of KRASG12D-dependent HPAFII cells with an IC50 of 78 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
No. CAS 2923669-20-7
-
Peso molecular 664.17
-
Fòrmula C37H35ClFN7O2
-
SMILES
ClC1=C(C(C2=C(C3=NC(C4=NC=C(N=C4)C)=C5C(N([C@@H]6[C@@H]7NC[C@H]6C7)C([C@H](N8C(COCC8)=O)C)=C5)=C3C=C2CCC#N)F)=CC=C1)C
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
INCB159020 Related Classifications
HY-168847 Related Classifications
Powered by Bioz