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

Rineterkib 

Cat. No.: HY-114491 Purity: 99.21% ee.: 98.91%
COA Handling Instructions

Rineterkib (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 Chemical Structure

Rineterkib Chemical Structure

CAS No. : 1715025-32-3

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 275 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 275 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 250 In-stock
Estimated Time of Arrival: December 31
10 mg USD 450 In-stock
Estimated Time of Arrival: December 31
25 mg USD 950 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2950 Get quote
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Rineterkib:

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 (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].

IC50 & Target[1]

ERK1

 

ERK2

 

RAF

 

In Vivo

Rineterkib (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
Molecular Weight

578.42

Appearance

Solid

Formula

C26H27BrF3N5O2
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
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 : 200 mg/mL (345.77 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7288 mL 8.6442 mL 17.2885 mL
5 mM 0.3458 mL 1.7288 mL 3.4577 mL
10 mM 0.1729 mL 0.8644 mL 1.7288 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 5 mg/mL (8.64 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:

Rineterkib1715025-32-3ERKRafExtracellular signal regulated kinasesRaf kinasesNSCLCKRASMAPKG12CG12DG12VInhibitorinhibitorinhibit

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