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.
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- CAS No.: 2923669-20-7
- Formule: C37H35ClFN7O2
- Masse moléculaire:664.17
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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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
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CAS No. 2923669-20-7
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Masse moléculaire 664.17
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Formule C37H35ClFN7O2
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
INCB159020 Related Classifications
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