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

Rineterkib 

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

Rineterkib (compound B) is an orally active RAF and ERK1/2 inhibitor in the study 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.

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 509 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 509 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 400 In-stock
Estimated Time of Arrival: December 31
10 mg USD 680 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1350 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

Rineterkib (compound B) is an orally active RAF and ERK1/2 inhibitor in the study 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[1].

IC50 & Target[1]

RAF

 

ERK1

 

ERK2

 

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.
Molecular Weight

578.42

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 provided by MCE.
References
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Keywords:

RineterkibRafERKRaf kinasesExtracellular signal regulated kinasesNSCLCKRASMAPKG12CG12DG12VInhibitorinhibitorinhibit

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Product Name:
Rineterkib
Cat. No.:
HY-114491
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