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

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

Rineterkib Chemical Structure

CAS No. : 1715025-32-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
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10 mg In-stock
25 mg In-stock
50 mg In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Rineterkib:

Rineterkib Related Antibodies

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:

View All Isoforms
B-Raf 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].

MedChemExpress (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.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(N[C@@H](C1=CC(F)=CC(Br)=C1)CNC)C2=CC=C(C3=NC([C@@H]4C[C@H](F)[C@@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 : 100 mg/mL (172.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.79%

SDS (252 KB)

COA (249 KB) LCMS (110 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7288 mL 8.6442 mL 17.2885 mL 43.2212 mL
5 mM 0.3458 mL 1.7288 mL 3.4577 mL 8.6442 mL
10 mM 0.1729 mL 0.8644 mL 1.7288 mL 4.3221 mL
15 mM 0.1153 mL 0.5763 mL 1.1526 mL 2.8814 mL
20 mM 0.0864 mL 0.4322 mL 0.8644 mL 2.1611 mL
25 mM 0.0692 mL 0.3458 mL 0.6915 mL 1.7288 mL
30 mM 0.0576 mL 0.2881 mL 0.5763 mL 1.4407 mL
40 mM 0.0432 mL 0.2161 mL 0.4322 mL 1.0805 mL
50 mM 0.0346 mL 0.1729 mL 0.3458 mL 0.8644 mL
60 mM 0.0288 mL 0.1441 mL 0.2881 mL 0.7204 mL
80 mM 0.0216 mL 0.1081 mL 0.2161 mL 0.5403 mL
100 mM 0.0173 mL 0.0864 mL 0.1729 mL 0.4322 mL
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Rineterkib Related Classifications

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.

Keywords:

Rineterkib1715025-32-3ERKRafExtracellular signal regulated kinasesRaf kinasesNSCLCKRASMAPKG12CG12DG12VInhibitorinhibitorinhibit

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