MedKoo Cat#: 406483 | Name: FLI-06
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Description:

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

FLI-06 is a Notch inhibitor and the early secretory pathway inhibitor. FLI-06 disrupts the Golgi apparatus in a manner distinct from that of brefeldin A and golgicide A. FLI-06 inhibits general secretion at a step before exit from the endoplasmic reticulum (ER), which was accompanied by a tubule-to-sheet morphological transition of the ER. FLI-06 is the first small molecule acting at such an early stage in secretory traffic. Notch signaling has a pivotal role in numerous cell-fate decisions, and its aberrant activity leads to developmental disorders and cancer.

Chemical Structure

FLI-06
FLI-06
CAS#313967-18-9

Theoretical Analysis

MedKoo Cat#: 406483

Name: FLI-06

CAS#: 313967-18-9

Chemical Formula: C25H30N2O5

Exact Mass: 438.2155

Molecular Weight: 438.52

Elemental Analysis: C, 68.47; H, 6.90; N, 6.39; O, 18.24

Price and Availability

Size Price Availability Quantity
10mg USD 350.00 2 Weeks
25mg USD 650.00 2 Weeks
50mg USD 950.00 2 Weeks
100mg USD 1,450.00 2 Weeks
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Related CAS #
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Synonym
FLI06; FLI 06; FLI06.
IUPAC/Chemical Name
cyclohexyl 2,7,7-trimethyl-4-(4-nitrophenyl)-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
InChi Key
SWWVFYHSSOWZMF-UHFFFAOYSA-N
InChi Code
InChI=1S/C25H30N2O5/c1-15-21(24(29)32-18-7-5-4-6-8-18)22(16-9-11-17(12-10-16)27(30)31)23-19(26-15)13-25(2,3)14-20(23)28/h9-12,18,22,26H,4-8,13-14H2,1-3H3
SMILES Code
O=C(C1=C(C)NC2=C(C(CC(C)(C)C2)=O)C1C3=CC=C([N+]([O-])=O)C=C3)OC4CCCCC4
Appearance
white 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
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Product Data
Safety Data Sheet (SDS)
Biological target:
FLI-06 is an inhibitor of Notch signaling with an EC50 of 2.3 μM.
In vitro activity:
The results showed that FLI-06 blocked proliferation, induced apoptosis and G1 phase arrest of ESCC cells in a dose-dependent manner. Mechanistically, this study found FLI-06 could inhibit Notch signaling pathway by decreasing the expressions of Notch3, DTX1 and Hes1. Reference: Biomed Pharmacother. 2018 Nov;107:1370-1376. https://pubmed.ncbi.nlm.nih.gov/30257352/
In vivo activity:
The results indicated that the body weights (Figure 4A) of the mice showed no variation, while the tumor volume (Figure 4B) and tumor weight (Figure 4C and D) of the FLI-06 treatment group were decreased compared with the control group. After treatment with FLI-06, the expression of Ki67 decreased, but the expression of Caspase-9 increased (Figure 4E and F) in xenograft tumors. Reference: Onco Targets Ther. 2019; 12: 7663–7674. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6756372/
Solvent mg/mL mM
Solubility
DMSO 45.0 102.53
DMF 20.0 45.61
DMF:PBS (pH 7.2) (1:4) 0.2 0.46
Ethanol 5.9 13.50
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 438.52 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:
1. Gan RH, Lin LS, Xie J, Huang L, Ding LC, Su BH, Peng XE, Zheng DL, Lu YG. FLI-06 Intercepts Notch Signaling And Suppresses The Proliferation And Self-renewal Of Tongue Cancer Cells. Onco Targets Ther. 2019 Sep 18;12:7663-7674. doi: 10.2147/OTT.S221231. PMID: 31571917; PMCID: PMC6756372. 2. Lu Z, Ren Y, Zhang M, Fan T, Wang Y, Zhao Q, Liu HM, Zhao W, Hou G. FLI-06 suppresses proliferation, induces apoptosis and cell cycle arrest by targeting LSD1 and Notch pathway in esophageal squamous cell carcinoma cells. Biomed Pharmacother. 2018 Nov;107:1370-1376. doi: 10.1016/j.biopha.2018.08.140. Epub 2018 Aug 31. PMID: 30257352.
In vitro protocol:
1. Gan RH, Lin LS, Xie J, Huang L, Ding LC, Su BH, Peng XE, Zheng DL, Lu YG. FLI-06 Intercepts Notch Signaling And Suppresses The Proliferation And Self-renewal Of Tongue Cancer Cells. Onco Targets Ther. 2019 Sep 18;12:7663-7674. doi: 10.2147/OTT.S221231. PMID: 31571917; PMCID: PMC6756372. 2. Lu Z, Ren Y, Zhang M, Fan T, Wang Y, Zhao Q, Liu HM, Zhao W, Hou G. FLI-06 suppresses proliferation, induces apoptosis and cell cycle arrest by targeting LSD1 and Notch pathway in esophageal squamous cell carcinoma cells. Biomed Pharmacother. 2018 Nov;107:1370-1376. doi: 10.1016/j.biopha.2018.08.140. Epub 2018 Aug 31. PMID: 30257352.
In vivo protocol:
1. Gan RH, Lin LS, Xie J, Huang L, Ding LC, Su BH, Peng XE, Zheng DL, Lu YG. FLI-06 Intercepts Notch Signaling And Suppresses The Proliferation And Self-renewal Of Tongue Cancer Cells. Onco Targets Ther. 2019 Sep 18;12:7663-7674. doi: 10.2147/OTT.S221231. PMID: 31571917; PMCID: PMC6756372.
1: Krämer A, Mentrup T, Kleizen B, Rivera-Milla E, Reichenbach D, Enzensperger C, Nohl R, Täuscher E, Görls H, Ploubidou A, Englert C, Werz O, Arndt HD, Kaether C. Small molecules intercept Notch signaling and the early secretory pathway. Nat Chem Biol. 2013 Nov;9(11):731-8. doi: 10.1038/nchembio.1356. Epub 2013 Sep 29. PubMed PMID: 24077179.