2. MAPK/ERK Pathway
    Stem Cell/Wnt
  3. ERK
    Raf
  4. Rineterkib hydrochloride

Rineterkib hydrochloride 

Cat. No.: HY-114491A Purity: 99.76% ee.: 98.91%
COA Handling Instructions

Rineterkib hydrochloride (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF.

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

Rineterkib hydrochloride Chemical Structure

Rineterkib hydrochloride Chemical Structure

CAS No. : 1715025-34-5

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Rineterkib hydrochloride:

Top Publications Citing Use of Products

View All ERK Isoform Specific Products:

View All Isoforms
ERK ERK1 ERK2 ERK5 ERK8

View All Raf Isoform Specific Products:

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BRaf c-Raf Raf

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Rineterkib hydrochloride (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF[1][2].

In Vivo

ERK-IN-1 (compound B) (50, 75 mg/kg, p.o., qd/q2d, 27 days) treatment significantly reduces the tumor volume in the Calu-6 human NSCLC subcutaneous tumor xenograft model in mice[1].

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

Animal Model: Calu-6 NSCLC xenograft tumor models in mice[1].
Dosage: 50, 75 mg/kg.
Administration: Orally either daily (qd) or every other day (q2d) for 27 days.
Result: Significantly reduced the tumor volume.
Clinical Trial
Appearance

Solid

Formula

C26H28BrClF3N5O2
CAS No.
SMILES

O=C(N[[email protected]@H](C1=CC(F)=CC(Br)=C1)CNC)C2=CC=C(C3=NC([[email protected]@H]4C[[email protected]](F)[[email protected]@H](O)CC4)=CN=C3N)C=C2F.[H]Cl.[x]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
In Vitro: 

DMSO : 220 mg/mL (Need ultrasonic)

In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 5.5 mg/mL (Infinity mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 5.5 mg/mL (Infinity mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 5.5 mg/mL (Infinity mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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Help & FAQs
  • 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.

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

Rineterkib1715025-34-5ERKRafExtracellular signal regulated kinasesRaf kinasesNSCLCKRASMAPKG12CG12DG12VInhibitorinhibitorinhibit

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