ChemicalBook > CAS DataBase List > FX1

FX1

Product Name
FX1
CAS No.
1426138-42-2
Chemical Name
FX1
Synonyms
FX1;CS-2497;FX-1;FX 1;FX1（CS-2497）;FX1 >=98% (HPLC);FX1, 10 mM in DMSO;inhibit,Apoptosis,Bcl-2 Family,FX 1,FX1,FX-1,Inhibitor;(Z)-3-(5-(5-chloro-2-oxoindolin-3-ylidene)-4-oxo-2-thioxothiazolidin-3-yl)propanoic acid;(5Z)-5-(5-Chloro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)-4-oxo-2-thioxo-3-thiazolidinepropanoic acid;3-Thiazolidinepropanoic acid, 5-(5-chloro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)-4-oxo-2-thioxo-, (5Z)-
CBNumber
CB03312337
Molecular Formula
C14H9ClN2O4S2
Formula Weight
368.82
MOL File
1426138-42-2.mol
More
Less

FX1 Property

storage temp. 
2-8°C
solubility 
DMSO:24.22(Max Conc. mg/mL);65.67(Max Conc. mM)
DMF:30.0(Max Conc. mg/mL);81.34(Max Conc. mM)
form 
powder
color 
white to beige
More
Less

Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

Precautionary statements

P280Wear protective gloves/protective clothing/eye protection/face protection.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

More
Less

N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML2074
Product name
FX1
Purity
≥98% (HPLC)
Packaging
5mg
Price
$102.38
Updated
2025/07/31
Sigma-Aldrich
Product number
SML2074
Product name
FX1
Purity
≥98% (HPLC)
Packaging
25mg
Price
$436
Updated
2025/07/31
Cayman Chemical
Product number
23908
Product name
FX1
Purity
≥95%
Packaging
1mg
Price
$32
Updated
2024/03/01
Cayman Chemical
Product number
23908
Product name
FX1
Purity
≥95%
Packaging
5mg
Price
$93
Updated
2024/03/01
Cayman Chemical
Product number
23908
Product name
FX1
Purity
≥95%
Packaging
10mg
Price
$169
Updated
2024/03/01
More
Less

FX1 Chemical Properties,Usage,Production

Uses

(5Z)-5-(5-Chloro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)-4-oxo-2-thioxo-3-thiazolidinepropanoic Acid is used in the preparation of substituted isatinylidenerhodanines. BCL6 inhibitor, an anticancer agent.

Definition

ChEBI: FX1 is a member of the class of oxindoles that is 5-chloro-oxindole in which the methylene hydrogens at position 3 have been replaced by an N-(2-carboxyethyl)rhodanin-5-ylidene group. It has a role as an antineoplastic agent. It is a member of oxindoles, an organochlorine compound, a thiazolidinone and a monocarboxylic acid. It is functionally related to a 3-methyleneoxindole and a rhodanine.

Biochem/physiol Actions

FX1 is a BCL6 inhibitor that effectively blocks BCL6 N-terminal BTB domain-mediated corepressors chromosome recruitment (by 61-87%/SMRT and 67-82%/BCOR; 50 μM FX1 for 30 min) and selectively suppresses BCL6-depenent growth (GI50 16-54 μM; >125 μM against BCL6-independent cells) in diffuse large B cell lymphoma (DLBCL) cultures, exhibiting greater affinity than its structure analog 79-6 or BCL6 corepressor SMRT for BTB domain (KD = 7 μM/FX1, 30 μM/SMRT, 129 μM/79-6). FX1 shows greater efficacy than 79-6 in reversing BCL6/corepressors-mediated target genes repression in vitro (IC50 = 35 μM vs. 318 μM with 79-6 by HEK293T-based reporter assay) and in suppressing OCI-Ly7 DLBCL xenograft tumor growth mice in vivo (100% vs. 45% suppression with respective compound via 25 mg/kg/day i.p.).

Synthesis

7025-19-6

17630-76-1

1426138-42-2

GENERAL METHOD: Acetic acid (5.0 mL) was added to a mixture of 5-chloroindole-2,3-dione (1.0 mmol), 3-(4-oxo-2-thioxothiazolidin-3-yl)propanoic acid (205 mg, 1.0 mmol) and sodium acetate (820 mg, 10.0 mmol). The reaction mixture was stirred at 105 °C for 30 min to 12 h, followed by cooling to room temperature. Water (15 mL) was added to the reaction system and the resulting mixture was sonicated to form an orange colored slurry. After filtration, the solid portion was washed with deionized water (75 mL) and dried under high vacuum to give the final target product (Z)-3-(5-(5-chloro-2-oxoindolin-3-ylidene)-4-oxo-2-thioxothiazolidin-3-yl)propionic acid as a red fine powder in 71-92% yield.

in vivo

Spleens in FX1-treating mice are macroscopically indistinguishable from vehicle controls. Total B cell abundance measured by flow cytometry is unaffected by FX1. GC B cells (GL7+FAS+B220+) are significantly depleted by exposure to FX1. Splenic architecture is examined by IHC. Staining with B220 antibody reveals normal B cell follicular structures, whereas staining for the GC B cell-specific marker peanut agglutinin shows profound loss of GCs. The half-life is estimated to be approximately 12 hours. Finally, whether FX1 can induce toxic effects in mice is assessed. 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 FX1 compare with vehicle[1].

storage

Store at -20°C

References

[1] Patent: WO2014/204859, 2014, A2. Location in patent: Page/Page column 34
[2] Tetrahedron Letters, 2013, vol. 54, # 13, p. 1700 - 1703

FX1 Preparation Products And Raw materials

Raw materials

Preparation Products

More
Less

FX1 Suppliers

China 87 India 1 United Kingdom 1 United States 8 USA 1 Global 98
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
Adamas Reagent, Ltd.
Tel
400-6009262 16621234537
Fax
021-64823266
Email
chenyj@titansci.com
Country
China
ProdList
14101
Advantage
59
Shanghai Topbiochem Technology Co., Ltd
Tel
021-58170097
Email
info@topbiochem.com
Country
China
ProdList
9510
Advantage
58
MedChemexpress LLC
Tel
021-58955995
Fax
609-228-5909
Email
sales@medchemexpress.cn
Country
United States
ProdList
4861
Advantage
58
EnliPharma Technology Co., Ltd
Tel
0551-66399836 18955197623
Email
sales@enlipharma.com
Country
China
ProdList
1876
Advantage
55
Shanghai JiYi Biotechnology Co. Ltd.
Tel
13621943973
Fax
-
Email
sales@shjiyipharmatech.com
Country
China
ProdList
1166
Advantage
55
Sigma-Aldrich
Tel
021-61415566 800-8193336
Email
orderCN@merckgroup.com
Country
China
ProdList
51395
Advantage
80
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4757
Advantage
55
Shanghaizehan biopharma technology co., Ltd.
Tel
021-61350663 13052117465
Fax
021-61350662
Email
sales@zehanbiopharma.com
Country
China
ProdList
984
Advantage
55
Shanghai EFE Biological Technology Co., Ltd.
Tel
021-65675885 18964387627
Fax
021-65675885
Email
info@efebio.com
Country
China
ProdList
9803
Advantage
58

1426138-42-2, FX1Related Search:


  • FX1
  • FX-1;FX 1
  • CS-2497
  • (Z)-3-(5-(5-chloro-2-oxoindolin-3-ylidene)-4-oxo-2-thioxothiazolidin-3-yl)propanoic acid
  • (5Z)-5-(5-Chloro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)-4-oxo-2-thioxo-3-thiazolidinepropanoic acid
  • 3-Thiazolidinepropanoic acid, 5-(5-chloro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)-4-oxo-2-thioxo-, (5Z)-
  • FX1 >=98% (HPLC)
  • inhibit,Apoptosis,Bcl-2 Family,FX 1,FX1,FX-1,Inhibitor
  • FX1（CS-2497）
  • 3-{5-[(3Z)-5-chloro-2-oxo-2,3-dihydro-1H-indol-3-ylidene]-4-oxo-2-thioxo-1,3-thiazol-3-yl}propanoic acid
  • FX1, 10 mM in DMSO
  • 1426138-42-2