2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. IACS-56676

IACS-56676 is a selective NRASG12D inhibitor with a target Kd of 0.031 μM. IACS-56676 stabilizes the p-loop, maintains key interactions with Asp12, Gly60 and Asp69, and achieves selectivity over wild-type KRAS through substitution targeting Leu95. IACS-56676 can be used for research on melanoma, hematologic malignancies and thyroid cancer.

For research use only. We do not sell to patients.

IACS-56676

IACS-56676 Chemical Structure

CAS No. : 3105153-34-9

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Description

IACS-56676 is a selective NRASG12D inhibitor with a target Kd of 0.031 μM. IACS-56676 stabilizes the p-loop, maintains key interactions with Asp12, Gly60 and Asp69, and achieves selectivity over wild-type KRAS through substitution targeting Leu95. IACS-56676 can be used for research on melanoma, hematologic malignancies and thyroid cancer[1].

In Vitro

IACS-56676 forms specific interactions with the NRASG12D protein, including a hydrogen bond with Glu62 and hydrophobic filling of the pocket formed by Leu95[1].
IACS-56676 potently inhibits NRASG12D target engagement in THP1 cells with an IC50 of 0.031 μM[1].
IACS-56676 potently reduces viability of NRASG12D-mutant THP1 cells with an IC50 of 0.073 μM[1].
IACS-56676 (up to 10 μM) has minimal CYP inhibition activity, with no measurable inhibition of CYP2D6 and CYP2C9 up to 10 μM, and weak inhibition of CYP3A4 isoforms[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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Molecular Weight

562.00

Formula

C28H28ClF4N5O
CAS No.
SMILES

NC1=CC(C2=C(F)C(N(C3CC3)C(CNC(C)=O)=C4[C@@]5([H])[C@@]6([H])[C@]5([H])CNC6)=C4C(C7CC7)=N2)=C(C(F)(F)F)C(Cl)=C1
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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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IACS-56676 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

IACS-566763105153-34-9IACS56676IACS 56676Rasthyroid carcinomasAsp12melanomaNRAS G12Dwild-type KRASTHP1 cellsLeu95Gly60Asp69hematologic malignanciesInhibitorinhibitorinhibit

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