Name: YK-4-279
Brand: Selleck Chemicals
SKU: S7679
Rating: 5 (14 reviews)

Hoppa till

Kvalitetskontroll (Quality Control)

Batch: Renhet: 99.93%

99.93

Relaterade mål	CDK HSP PD-1/PD-L1 ROCK Wee1 Microtubule Associated Ras KRas Aurora Kinase Casein Kinase
Övrigt DNA/RNA Synthesis Inhibitorer	CX-5461 (Pidnarulex) SCR7 Favipiravir (T-705) RK-33 EED226 BMH-21 Carmofur Triapine (3-AP) Halofuginone Tegafur (FT-207)

Cellodling, behandling & arbetskoncentration
(Cell Culture, Treatment & Working Concentration)

Cellinjer	Analystyp	Inkubationstid	Aktivitetsbeskrivning	PMID
COS7	Function assay		Inhibition of transcriptional activity of full-length EWS-FLI1 (unknown origin) expressed in COS7 cells by NR0B1-luciferase reporter gene assay, IC50=0.35μM	25432018
TC71	Growth inhibition assay	3 days	Growth inhibition of human TC71 cells harboring EWS-FLI1 fusion protein after 3 days by WST1 assay, GI50=0.92μM	25432018
TC32	Growth inhibition assay	3 days	Growth inhibition of human TC32 cells harboring EWS-FLI1 fusion protein after 3 days by WST1 assay, GI50=0.94μM	25432018
TC32	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
DAOY	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
SJ-GBM2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
A673	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB-EBc1	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
Saos-2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
LAN-5	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
BT-12	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
OHS-50	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
RD	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
MG 63 (6-TG R)	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
Rh41	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
Klicka för att visa mer experimentella data för cellinjer

Kemisk information, lagring & stabilitet (Chemical Information, Storage & Stability)

Molekylvikt	366.20	Formel	C₁₇H₁₃Cl₂NO₄	Lagring (från mottagningsdatumet)	3 år-20°Cpulver
CAS-nr	1037184-44-3	Ladda ner SDF		Lagring av stamlösningar	1 år-80°Ci lösningsmedel 1 månad-20°Ci lösningsmedel
Synonymer	N/A			Smiles	COC1=CC=C(C=C1)C(=O)CC2(C3=C(C=CC(=C3NC2=O)Cl)Cl)O

Löslighet (Solubility)

In vitro
Batch:

DMSO : 73 mg/mL (199.34 mM)
(Fuktkontaminerad DMSO kan minska lösligheten. Använd färk, vattenfri DMSO.)

Ethanol : 73 mg/mL

Water : Insoluble

Molaritetsräknare

Massa	Koncentration	Volym	Molekylvikt
=	×	×

Utspädningsräknare Molekylviktsräknare

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 Validerad av Selleck-laboratorier. Om du behöver justeringar av denna formulering, kontakta vårt säljteam för skräddarsydd testning.	3.650mg/ml (9.97mM)	Taking the 1 mL working solution as an example, add 50 μL of 73 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL 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 Validerad av Selleck-laboratorier. Om du behöver justeringar av denna formulering, kontakta vårt säljteam för skräddarsydd testning.	0.600mg/ml (1.64mM)	Taking the 1 mL working solution as an example, add 50 μL of 12 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-formuleringsräknare (Klar lösning)

Steg 1: Ange information nedan (Rekommenderas: Ett extra djur för att ta hänsyn till förluster under experimentet)

Dosering: mg/kg Djurens medelvikt: g Doseringsvolym per djur:μL Antal djur:

Steg 2: Ange in vivo-formuleringen (Detta är endast räknaren, inte formuleringen. Vänligen kontakta oss först om det inte finns någon in vivo-formulering i löslighetsavsnittet.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Beräkningsresultat:

Arbetskoncentration: mg/ml;

Metod för att bereda DMSO-stamlösning: mg substans förlöst i μL DMSO ( Stamlösningskoncentration mg/mL, Vänligen kontakta oss först om koncentrationen överskrider DMSO-lösligheten för denna batch av substansen. )

Metod för att bereda in vivo-formulering: Ta μL DMSO stamlösning, tillsätt sedanμL PEG300, blanda och klarna, tillsätt sedanμL Tween 80, blanda och klarna, tillsätt sedan μL ddH₂O, blanda och klarna.

Metod för att bereda in vivo-formulering: Ta μL DMSO stamlösning, tillsätt sedan μL Majsolja, blanda och klarna.

Obs: 1. Se till att vätskan är klar innan du tillsätter nästa lösningsmedel.
2. Se till att tillsätta lösningsmedlet/lösningsmedlen i ordning. Du måste se till att lösningen som erhålls i föregående tillsats är en klar lösning innan du fortsätter att tillsätta nästa lösningsmedel. Fysiska metoder som vortex, ultraljud eller varmt vattenbad kan användas för att underlätta upplösningen.

Verkningsmekanism (Mechanism of Action)

Targets/IC₅₀/Ki	RHA
In vitro	YK-4-279 eliminates cyclin D levels by blocking the interaction of EWS-FLI1 with RHA in EWS-FLI1-containing TC32 cells. This compound also specifically inhibits ESFT cell growth and induces apoptosis. It also inhibits ERG and ETV1 biological activity in fusion-positive prostate cancer cells, and further decreases cell motility and invasion.
In vivo	In vivo, YK-4-279 (1.5 mg/dose i.p.) inhibits the growth of ESFT xenograft tumors. In mouse model, this compound selectively prevents prostate cancer growth and metastasis in fusion-positive LNCaP-luc-M6 tumors.
Referenser	[1] https://pubmed.ncbi.nlm.nih.gov/19584866/ [2] https://pubmed.ncbi.nlm.nih.gov/21559405/ [3] https://pubmed.ncbi.nlm.nih.gov/25479232/

Applikationer (Applications)

Metoder	Biomarkörer	Bilder	PMID
Growth inhibition assay	Cell viability		29212266
Western blot	PARP / Cleaved PARP / Caspase 3 / Cleaved Caspase 3 p-HH3(Ser10) / Histone H3 / p-Aurora A (T288) / Aurora A / Aurora B / Cyclin B / p53 / p21		29212266

Vanliga frågor (Frequently Asked Questions)

Fråga 1:
I would like to know whether it is the racemate version, or whether it is the + R-enantiomer or the – S-enantiomer of this compound?

Svar:
For our S7679, it is a recemate.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

YK-4-279 DNA/RNA Synthesis Hämmare

Molekylvikt: 366.20

Kvalitetskontroll (Quality Control)

Cellodling, behandling & arbetskoncentration
(Cell Culture, Treatment & Working Concentration)

Kemisk information, lagring & stabilitet (Chemical Information, Storage & Stability)

Löslighet (Solubility)

Molaritetsräknare

In vivo-formuleringsräknare (Klar lösning)

Verkningsmekanism (Mechanism of Action)

Applikationer (Applications)

Vanliga frågor (Frequently Asked Questions)

YK-4-279 DNA/RNA Synthesis Hämmare

Molekylvikt: 366.20

Kvalitetskontroll (Quality Control)

Cellodling, behandling & arbetskoncentration (Cell Culture, Treatment & Working Concentration)

Kemisk information, lagring & stabilitet (Chemical Information, Storage & Stability)

Löslighet (Solubility)

Molaritetsräknare

In vivo-formuleringsräknare (Klar lösning)

Verkningsmekanism (Mechanism of Action)

Applikationer (Applications)

Vanliga frågor (Frequently Asked Questions)

Cellodling, behandling & arbetskoncentration
(Cell Culture, Treatment & Working Concentration)