MedKoo Cat#: 462502 | Name: Rineterkib free base
Featured New

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Rineterkib, also known as LTT-462 or ERK-IN-1, is a ERK1/2 inhibitor which has demonstrated preclinical activity in multiple MAPK activated cancer cells and xenograft models. LTT462 binds to and inhibits ERK, thereby preventing the activation of ERK-mediated signal transduction pathways. This results in the inhibition of ERK-dependent tumor cell proliferation and survival. The mitogen-activated protein kinase (MAPK)/ERK pathway is upregulated in numerous tumor cell types and plays a key role in tumor cell proliferation, differentiation and survival.

Chemical Structure

Rineterkib free base
Rineterkib free base
CAS#1715025-32-3 (free base)

Theoretical Analysis

MedKoo Cat#: 462502

Name: Rineterkib free base

CAS#: 1715025-32-3 (free base)

Chemical Formula: C26H27BrF3N5O2

Exact Mass: 577.1300

Molecular Weight: 578.43

Elemental Analysis: C, 53.99; H, 4.71; Br, 13.81; F, 9.85; N, 12.11; O, 5.53

Price and Availability

Size Price Availability Quantity
1mg USD 90.00 Ready to ship
5mg USD 250.00 Ready to ship
10mg USD 450.00 Ready to ship
25mg USD 950.00 Ready to ship
50mg USD 1,650.00 Ready to ship
100mg USD 2,950.00 Ready to ship
Show More
Bulk Inquiry
Buy Now
Add to Cart
Synonym
Rineterkib; ERK-IN-1; ERK IN 1; ERK IN-1; ERK-IN 1; LTT 462; LTT-462; LTT462;
IUPAC/Chemical Name
4-{3-amino-6-[(1S,3S,4S)-3-fluoro-4-hydroxycyclohexyl]pyrazin-2-yl}-N-[(1S)-1-(3-bromo-5-fluorophenyl)-2-(methylamino)ethyl]-2-fluorobenzamide
InChi Key
YFCIFWOJYYFDQP-PTWZRHHISA-N
InChi Code
InChI=1S/C26H27BrF3N5O2/c1-32-11-21(15-6-16(27)10-17(28)7-15)35-26(37)18-4-2-14(9-19(18)29)24-25(31)33-12-22(34-24)13-3-5-23(36)20(30)8-13/h2,4,6-7,9-10,12-13,20-21,23,32,36H,3,5,8,11H2,1H3,(H2,31,33)(H,35,37)/t13-,20-,21+,23-/m0/s1
SMILES Code
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
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Biological target:
Rineterkib (compound B) is an active RAF and ERK1/2 inhibitor in the study of a proliferative disease characterized by activating mutations in the MAPK pathway.
In vitro activity:
TBD
In vivo activity:
TBD
Solvent mg/mL mM
Solubility
DMSO 0.0 0.00
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 578.43 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
TBD
In vitro protocol:
TBD
In vivo protocol:
TBD
Planchard, D., Wolf, J., Solomon, B., Sebastian, M., Wermke, M., Heist, R. S., ... & Dooms, C. (2024). A phase Ib study of the combination of naporafenib with rineterkib or trametinib in patients with advanced and metastatic KRAS-or BRAF-mutant non-small cell lung cancer. Lung Cancer, 107964.