MedKoo Cat#: 207057 | Name: Rineterkib mesylate

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 RAF and 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 mesylate
Rineterkib mesylate
CAS#Rineterkib mesylate

Theoretical Analysis

MedKoo Cat#: 207057

Name: Rineterkib mesylate

CAS#: Rineterkib mesylate

Chemical Formula: C28H35BrF3N5O8S2

Exact Mass: 0.0000

Molecular Weight: 770.63

Elemental Analysis: C, 43.64; H, 4.58; Br, 10.37; F, 7.40; N, 9.09; O, 16.61; S, 8.32

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Synonym
LTT462; LTT-462; LTT 462; Rineterkib mesylate; Rineterkib dimesylate;
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 dimesylate
InChi Key
JNVGCRHDQZIQCB-UQNNFWOVSA-N
InChi Code
InChI=1S/C26H27BrF3N5O2.2CH4O3S/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;2*1-5(2,3)4/h2,4,6-7,9-10,12-13,20-21,23,32,36H,3,5,8,11H2,1H3,(H2,31,33)(H,35,37);2*1H3,(H,2,3,4)/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.OS(=O)(C)=O.OS(=O)(C)=O
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

Preparing Stock Solutions

The following data is based on the product molecular weight 770.63 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
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.