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FX1 Bcl-6 inhibitor

Name: FX1
Brand: Selleck Chemicals
SKU: S8591
Availability: InStock
Rating: 5 (11 reviews)

Cat.No.S8591

FX1 is a selective BCL6 BTB inhibitor with an IC50 value of 35 μM in reporter assays. This compound shows great selectivity against a panel of 50 different kinases. 10 μM of this chemical fails to significantly inhibit of any of these kinases. It induces apoptosis.

Chemical Structure

Molecular Weight: 368.82

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.75%

99.75

Related Targets	Apoptosis related Ras STAT TNF-alpha Bcl-2 Caspase PD-1/PD-L1 Ferroptosis p53 RIP kinase c-RET MDM2/MDMX Myc IAP OXPHOS PERK FKBP Thymidylate Synthase ABC Transporter Heme Oxygenase PFKFB Pyroptosis PKD Survivin ASK Nur77 DAPK TRADD TACE Cuproptosis
Related Products	79-6 (CID5721353) BI-3812 BI-3802 BCL6 Antibody [B14D22] BCL6 Antibody [L21J6]

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
TMD8	Antiproliferative assay	3 days	Antiproliferative activity against BCL6 dependent human TMD8 cells after 3 days by CellTiter-Glo assay, GI50 = 10 μM.	28485934
SUDHL4	Antiproliferative assay	3 days	Antiproliferative activity against BCL6 dependent human SUDHL4 cells after 3 days by CellTiter-Glo assay, GI50 = 10 μM.	28485934
OCI-LY19	Antiproliferative assay	3 days	Antiproliferative activity against BCL6 independent human OCI-LY19 cells after 3 days by CellTiter-Glo assay, GI50 = 10 μM.	28485934
OCI-LY10	Antiproliferative assay	3 days	Antiproliferative activity against BCL6 dependent human OCI-LY10 cells after 3 days by CellTiter-Glo assay, GI50 = 12.5892 μM.	28485934
SU-DHL-2	Antiproliferative assay	3 days	Antiproliferative activity against BCL6 dependent human SU-DHL-2 cells after 3 days by CellTiter-Glo assay, GI50 = 12.5892 μM.	28485934
U2932	Antiproliferative assay	3 days	Antiproliferative activity against BCL6 dependent human U2932 cells after 3 days by CellTiter-Glo assay, GI50 = 12.5892 μM.	28485934
KARPAS422	Antiproliferative assay	3 days	Antiproliferative activity against BCL6 independent human KARPAS422 cells after 3 days by CellTiter-Glo assay, GI50 = 12.5892 μM.	28485934
OCI-LY1	Antiproliferative assay	3 days	Antiproliferative activity against BCL6 dependent human OCI-LY1 cells after 3 days by CellTiter-Glo assay, GI50 = 19.9526 μM.	28485934
OCI-LY3	Antiproliferative assay	3 days	Antiproliferative activity against BCL6 dependent human OCI-LY3 cells after 3 days by CellTiter-Glo assay, GI50 = 19.9526 μM.	28485934
AMO1	Antiproliferative assay	3 days	Antiproliferative activity against BCL6 dependent human AMO1 cells after 3 days by CellTiter-Glo assay, GI50 = 19.9526 μM.	28485934
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	368.82	Formula	C₁₄H₉ClN₂O₄S₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1426138-42-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1=CC2=NC(=O)C(=C2C=C1Cl)C3=C(N(C(=S)S3)CCC(=O)O)O

Solubility

In vitro
Batch:

DMSO : 20 mg/mL (54.22 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 37 mg/mL (100.31 mM) Warmed with 50°C water bath; Ultrasonicated;
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.900mg/ml (2.44mM)	Taking the 1 mL working solution as an example, add 50 μL of 18 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.300mg/ml (0.81mM)	Taking the 1 mL working solution as an example, add 50 μL of 6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Features	Recommend for freshly prepared each time for in vitro experiment
Targets/IC₅₀/Ki	BCL6 BTB ^[1] (Cell-free assay) 35 μM
In vitro	FX1 disrupted formation of the BCL6 repression complex, reactivated BCL6 target genes, and mimicked the phenotype of mice engineered to express BCL6 with corepressor binding site mutations. This compound suppressed ABC-DLBCL cells in vitro and in vivo, as well as primary human ABC-DLBCL specimens ex vivo. It is specific to BCL6 and binds with a greater affinity than the natural BCL6 ligand SMRT. This chemical almost invariantly induced significant derepression of these genes(BCL6 target genes CASP8, CD69, CXCR4, CDKN1A, and DUSP5) as compared with vehicle in 2 independent DLBCL cell lines. It was more than 100-fold more powerful than the previous generation of BCL6 inhibitors represented by 79-6, and 300-fold more potent than the recently reported binding of the antibiotics rifamycin and rifabutin (KD ~1 mM)^[1].
In vivo	Low doses of FX1 induce regression of established tumors in mice bearing DLBCL xenografts. The half-life is estimated to be approximately 12 hours for this compound in SCID mice. No signs of toxicity, inflammation, or infection are evident from H&E-stained sections of lung, gastrointestinal tract, heart, kidney, liver, spleen, and bone marrow of the fixed organs from mice treated with this chemical compared with vehicle. Peripheral blood counts and serum chemistry in FX1-treated mice are also examined and they remain within normal parameters. This compound causes profound and significant suppression of DLBCLs in DLBCL xenografts, and indeed not only prevented growth of the xenografts but in addition causes these tumors to shrink from their initial volume. The maximal effect is already achieved by the lower 25 mg/kg dose. TUNEL and Ki-67 staining shows that this agent also induced more apoptosis and growth arrest than 79-6, respectively^[1].
References	[1] https://pubmed.ncbi.nlm.nih.gov/27482887/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02902679	Completed	Thrombosis\|Factor XI\|Renal Impairment\|ESRD (End-Stage Renal Disease)	Bristol-Myers Squibb	November 2016	Phase 1

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