FDI-6 | CAS#313380-27-7 | FOXM1 inhibitor

FDI-6
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 562568

CAS#: 313380-27-7

Description: FDI-6 is an inhibitor of FOXM1 that block DNA binding. It act by specifically downregulating FOXM1-activated genes with FOXM1 occupancy confirmed by ChIP-PCR.

Chemical Structure

FDI-6

CAS# 313380-27-7

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 562568
Name: FDI-6
CAS#: 313380-27-7
Chemical Formula: C19H11F4N3OS2
Exact Mass: 437.03
Molecular Weight: 437.430
Elemental Analysis: C, 52.17; H, 2.53; F, 17.37; N, 9.61; O, 3.66; S, 14.66

Price and Availability

Size	Price	Availability
5mg	USD 240	2 weeks
25mg	USD 600	2 weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: FDI-6; FDI 6; FDI6; NCGC00099374; NCGC-00099374; NCGC 00099374;

IUPAC/Chemical Name: 3-Amino-N-(4-fluorophenyl)-6-thiophen-2-yl-4-(trifluoromethyl)thieno[2,3-b]pyridine-2-carboxamide

InChi Key: ZATJMMZPGVDUOM-UHFFFAOYSA-N

InChi Code: InChI=1S/C19H11F4N3OS2/c20-9-3-5-10(6-4-9)25-17(27)16-15(24)14-11(19(21,22)23)8-12(26-18(14)29-16)13-2-1-7-28-13/h1-8H,24H2,(H,25,27)

SMILES Code: O=C(C1=C(N)C2=C(C(F)(F)F)C=C(C3=CC=CS3)N=C2S1)NC4=CC=C(F)C=C4

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: >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:

Product Data

Instruction:

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Biological target:	FDI-6 is an inhibitor of FOXM1.
In vitro activity:	This study then investigated the anti-proliferative effect of FDI-6 using a Sulforhodamine B (SRB) assay. The results demonstrated that FDI-6 inhibits cell proliferation in a dose-dependent manner. Reference: Int J Mol Sci. 2021 Jun 22;22(13):6685. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8269391/
In vivo activity:	In vivo, FDI-6 (40 μM) was injected subconjunctivally to a rabbit trabeculectomy model. The results showed that, in cell culture studies, FDI-6 suppressed the proliferation, migration, collagen gel contraction and the expression levels of fibronectin (FN) and α-smooth muscle actin (α-SMA) in RTFs with TGF-β treatment by down-regulating the TGF-β1/Smad2/3 signaling pathway. In animal studies, the IOPs of the FDI-6-treated group were significantly lower than those of the saline-treated group after trabeculectomy. The FDI-6-treated eyes showed a better bleb appearance with fewer blood vessels compared to the saline-treated eyes. Reference: Exp Eye Res. 2021 Aug 7:108725. https://pubmed.ncbi.nlm.nih.gov/34375589/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	64.3	147.09

Preparing Stock Solutions

The following data is based on the product molecular weight 437.43 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.

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. Ulhaka K, Kanokwiroon K, Khongkow M, Bissanum R, Khunpitak T, Khongkow P. The Anticancer Effects of FDI-6, a FOXM1 Inhibitor, on Triple Negative Breast Cancer. Int J Mol Sci. 2021 Jun 22;22(13):6685. doi: 10.3390/ijms22136685. PMID: 34206484; PMCID: PMC8269391. 2. Liu Y, Zhu L, Wen T, Wan J, Lei Y, Chen H. [Forkhead domain inhibitor-6 (FDI-6) increases apoptosis and inhibits invasion and migration of laryngeal carcinoma cells by down-regulating nuclear FoxM1]. Xi Bao Yu Fen Zi Mian Yi Xue Za Zhi. 2017 May;33(5):611-616. Chinese. PMID: 28502298. 3. Lan C, Tan J, Tang L, Liu G, Huang L, Luo X, Zhou L, Zhu Y, Liu X, Fan N. Forkhead domain inhibitory-6 attenuates subconjunctival fibrosis in rabbit model with trabeculectomy. Exp Eye Res. 2021 Aug 7:108725. doi: 10.1016/j.exer.2021.108725. Epub ahead of print. PMID: 34375589.
In vitro protocol:	1. Ulhaka K, Kanokwiroon K, Khongkow M, Bissanum R, Khunpitak T, Khongkow P. The Anticancer Effects of FDI-6, a FOXM1 Inhibitor, on Triple Negative Breast Cancer. Int J Mol Sci. 2021 Jun 22;22(13):6685. doi: 10.3390/ijms22136685. PMID: 34206484; PMCID: PMC8269391. 2. Liu Y, Zhu L, Wen T, Wan J, Lei Y, Chen H. [Forkhead domain inhibitor-6 (FDI-6) increases apoptosis and inhibits invasion and migration of laryngeal carcinoma cells by down-regulating nuclear FoxM1]. Xi Bao Yu Fen Zi Mian Yi Xue Za Zhi. 2017 May;33(5):611-616. Chinese. PMID: 28502298.
In vivo protocol:	1. Lan C, Tan J, Tang L, Liu G, Huang L, Luo X, Zhou L, Zhu Y, Liu X, Fan N. Forkhead domain inhibitory-6 attenuates subconjunctival fibrosis in rabbit model with trabeculectomy. Exp Eye Res. 2021 Aug 7:108725. doi: 10.1016/j.exer.2021.108725. Epub ahead of print. PMID: 34375589.

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1: Tabatabaei-Dakhili SA, Aguayo-Ortiz R, Domínguez L, Velázquez-Martínez CA. Untying the knot of transcription factor druggability: Molecular modeling study of FOXM1 inhibitors. J Mol Graph Model. 2018 Mar;80:197-210. doi: 10.1016/j.jmgm.2018.01.009. Epub 2018 Jan 31. PubMed PMID: 29414039.

2: Otto-Duessel M, Tew BY, Vonderfecht S, Moore R, Jones JO. Identification of neuron selective androgen receptor inhibitors. World J Biol Chem. 2017 May 26;8(2):138-150. doi: 10.4331/wjbc.v8.i2.138. PubMed PMID: 28588757; PubMed Central PMCID: PMC5439165.

3: Liu Y, Zhu L, Wen T, Wan J, Lei Y, Chen H. [Forkhead domain inhibitor-6 (FDI-6) increases apoptosis and inhibits invasion and migration of laryngeal carcinoma cells by down-regulating nuclear FoxM1]. Xi Bao Yu Fen Zi Mian Yi Xue Za Zhi. 2017 May;33(5):611-616. Chinese. PubMed PMID: 28502298.

4: Youn M, Wang N, LaVasseur C, Bibikova E, Kam S, Glader B, Sakamoto KM, Narla A. Loss of Forkhead box M1 promotes erythropoiesis through increased proliferation of erythroid progenitors. Haematologica. 2017 May;102(5):826-834. doi: 10.3324/haematol.2016.156257. Epub 2017 Feb 2. PubMed PMID: 28154085; PubMed Central PMCID: PMC5477601.

5: Marsico G, Gormally MV. Small molecule inhibition of FOXM1: How to bring a novel compound into genomic context. Genom Data. 2014 Oct 22;3:19-23. doi: 10.1016/j.gdata.2014.10.012. eCollection 2015 Mar. PubMed PMID: 26484143; PubMed Central PMCID: PMC4535965.

6: Kalinichenko VV, Kalin TV. Is there potential to target FOXM1 for 'undruggable' lung cancers? Expert Opin Ther Targets. 2015 Jul;19(7):865-7. doi: 10.1517/14728222.2015.1042366. Epub 2015 May 4. PubMed PMID: 25936405; PubMed Central PMCID: PMC4836176.

7: Gormally MV, Dexheimer TS, Marsico G, Sanders DA, Lowe C, Matak-Vinković D, Michael S, Jadhav A, Rai G, Maloney DJ, Simeonov A, Balasubramanian S. Suppression of the FOXM1 transcriptional programme via novel small molecule inhibition. Nat Commun. 2014 Nov 12;5:5165. doi: 10.1038/ncomms6165. PubMed PMID: 25387393; PubMed Central PMCID: PMC4258842.

8: Ridding MC, Taylor JL, Rothwell JC. The effect of voluntary contraction on cortico-cortical inhibition in human motor cortex. J Physiol. 1995 Sep 1;487 ( Pt 2):541-8. PubMed PMID: 8558482; PubMed Central PMCID: PMC1156591.

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