LJI308 | CAS#1627709-94-7 | RSK inhibitor

MedKoo Cat#: 407301 | Name: LJI308

Description:

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

LJI308 is a RSK inhibitor. LJI308 overcomes chemoresistance by eliminating cancer stem cells. LJI308 targets the CSC population and repress TNBC growth and dissemination. LJI308 specifically targeted transformed cells as it had little effect on the non-tumorigenic parental HMECs. Targeting RSK using specific and potent inhibitors, such as LJI308, delivers the promise of inhibiting the growth of TNBC.

Chemical Structure

LJI308

CAS#1627709-94-7

Theoretical Analysis

MedKoo Cat#: 407301

Name: LJI308

CAS#: 1627709-94-7

Chemical Formula: C21H18F2N2O2

Exact Mass: 368.1336

Molecular Weight: 368.38

Elemental Analysis: C, 68.47; H, 4.93; F, 10.31; N, 7.60; O, 8.69

Price and Availability

Size	Price	Availability
50mg	USD 450.00	2 Weeks
100mg	USD 750.00	2 Weeks
200mg	USD 1,250.00	2 Weeks
500mg	USD 2,450.00	2 Weeks
1g	USD 3,850.00	2 Weeks
2g	USD 5,950.00	2 Weeks

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Synonym

LJI308; LJI-308; LJI 308; NVP-LJI308; NVP-LJI-308; NVP-LJI 308.

IUPAC/Chemical Name

2,6-Difluoro-4-[4-[4-(4-morpholinyl)phenyl]-3-pyridinyl]-phenol

InChi Key

YUYJEQHNWKQNBT-UHFFFAOYSA-N

InChi Code

InChI=1S/C21H18F2N2O2/c22-19-11-15(12-20(23)21(19)26)18-13-24-6-5-17(18)14-1-3-16(4-2-14)25-7-9-27-10-8-25/h1-6,11-13,26H,7-10H2

SMILES Code

OC1=C(F)C=C(C2=C(C3=CC=C(N4CCOCC4)C=C3)C=CN=C2)C=C1F

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, not in water

Shelf Life

>2 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

Product Data

Product Data

Instruction

View handling instruction

Biological target:

LJI308 is a potent pan-ribosomal S6 kinase (RSK) inhibitor, with IC50s of 6 nM, 4 nM, and 13 nM for RSK1, RSK2, and RSK3, respectively.

In vitro activity:

LJI308 inhibited the phosphorylation of RSK (T359/S363) and YB-1 (S102) after irradiation, treatment with EGF, and in cells expressing a KRAS mutation. LJI308 treatment slightly inhibited DSB repair only in some of the cell lines tested. Reference: Int J Radiat Oncol Biol Phys. 2021 Feb 1;109(2):567-580. https://pubmed.ncbi.nlm.nih.gov/32931865/

In vivo activity:

TBD

	Solvent	mg/mL	mM
Solubility
	DMF	10.0	27.15
	DMSO	17.8	48.34
	DMSO:PBS (pH 7.2) (1:9)	0.1	0.27

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 368.38 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.

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:

1. Lettau K, Zips D, Toulany M. Simultaneous Targeting of RSK and AKT Efficiently Inhibits YB-1-Mediated Repair of Ionizing Radiation-Induced DNA Double-Strand Breaks in Breast Cancer Cells. Int J Radiat Oncol Biol Phys. 2021 Feb 1;109(2):567-580. doi: 10.1016/j.ijrobp.2020.09.005. Epub 2020 Sep 12. PMID: 32931865. 2. Davies AH, Reipas K, Hu K, Berns R, Firmino N, Stratford AL, Dunn SE. Inhibition of RSK with the novel small-molecule inhibitor LJI308 overcomes chemoresistance by eliminating cancer stem cells. Oncotarget. 2015 Aug 21;6(24):20570-7. doi: 10.18632/oncotarget.4135. PMID: 26011941; PMCID: PMC4653026.

In vitro protocol:

In vivo protocol:

TBD

1: Davies AH, Reipas K, Hu K, Berns R, Firmino N, Stratford AL, Dunn SE. Inhibition of RSK with the novel small-molecule inhibitor LJI308 overcomes chemoresistance by eliminating cancer stem cells. Oncotarget. 2015 Aug 21;6(24):20570-7. PubMed PMID: 26011941; PubMed Central PMCID: PMC4653026. 2: Aronchik I, Appleton BA, Basham SE, Crawford K, Del Rosario M, Doyle LV, Estacio WF, Lan J, Lindvall MK, Luu CA, Ornelas E, Venetsanakos E, Shafer CM, Jefferson AB. Novel potent and selective inhibitors of p90 ribosomal S6 kinase reveal the heterogeneity of RSK function in MAPK-driven cancers. Mol Cancer Res. 2014 May;12(5):803-12. doi: 10.1158/1541-7786.MCR-13-0595. Epub 2014 Feb 19. PubMed PMID: 24554780.