NSC745885
Based on 1 Customer Validation
NSC745885 an effective anti-tumor agent, shows selective toxicity against multiple cancer cell lines but not normal cells. NSC745885 is an effective down-regulator of EZH2 via proteasome-mediated degradation. NSC745885 provides possibilities for the study of advanced bladder and oral squamous cell carcinoma (OSCC) cancers.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 98.0%
- CAS No.: 4219-52-7
- Formule: C14H6N2O2S
- Masse moléculaire:266.27
-
Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
Description
IC50 & Target
[2]|
EZH2 |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| 786-0 | GI50 |
6.17 μM
Compound: 23, NSC-745885
|
Growth inhibition of human 786-0 cells
Growth inhibition of human 786-0 cells
|
[PMID: 19804981] |
| A498 | GI50 |
12.4 μM
Compound: 23, NSC-745885
|
Growth inhibition of human A498 cells
Growth inhibition of human A498 cells
|
[PMID: 19804981] |
| A549 | GI50 |
14.7 μM
Compound: 23, NSC-745885
|
Growth inhibition of human A549 cells
Growth inhibition of human A549 cells
|
[PMID: 19804981] |
| ACHN | GI50 |
1.46 μM
Compound: 23, NSC-745885
|
Growth inhibition of human ACHN cells
Growth inhibition of human ACHN cells
|
[PMID: 19804981] |
| BT-549 | GI50 |
1.63 μM
Compound: 23, NSC-745885
|
Growth inhibition of human BT549 cells
Growth inhibition of human BT549 cells
|
[PMID: 19804981] |
| CAKI-1 | GI50 |
1.61 μM
Compound: 23, NSC-745885
|
Growth inhibition of human Caki1 cells
Growth inhibition of human Caki1 cells
|
[PMID: 19804981] |
| CCRF-CEM | GI50 |
1.08 μM
Compound: 23, NSC-745885
|
Growth inhibition of human CCRF-CEM cells
Growth inhibition of human CCRF-CEM cells
|
[PMID: 19804981] |
| COLO 205 | GI50 |
13.4 μM
Compound: 23, NSC-745885
|
Growth inhibition of human COLO205 cells
Growth inhibition of human COLO205 cells
|
[PMID: 19804981] |
| DU-145 | GI50 |
1.67 μM
Compound: 23, NSC-745885
|
Growth inhibition of human DU145 cells
Growth inhibition of human DU145 cells
|
[PMID: 19804981] |
| DU-145 | IC50 |
7.41 μM
Compound: 2, NSC745885
|
Cytotoxicity against human DU145 cells after 72 hrs by MTT assay
Cytotoxicity against human DU145 cells after 72 hrs by MTT assay
|
[PMID: 26344783] |
| EKVX | GI50 |
1.55 μM
Compound: 23, NSC-745885
|
Growth inhibition of human EKVX cells
Growth inhibition of human EKVX cells
|
[PMID: 19804981] |
| HCC 2998 | GI50 |
16.4 μM
Compound: 23, NSC-745885
|
Growth inhibition of human HCC2998 cells
Growth inhibition of human HCC2998 cells
|
[PMID: 19804981] |
| HCT-116 | GI50 |
1.93 μM
Compound: 23, NSC-745885
|
Growth inhibition of human HCT116 cells
Growth inhibition of human HCT116 cells
|
[PMID: 19804981] |
| HCT-15 | GI50 |
1.71 μM
Compound: 23, NSC-745885
|
Growth inhibition of human HCT15 cells
Growth inhibition of human HCT15 cells
|
[PMID: 19804981] |
| HL-60(TB) | GI50 |
0.16 μM
Compound: 23, NSC-745885
|
Growth inhibition of human HL-60(TB) cells
Growth inhibition of human HL-60(TB) cells
|
[PMID: 19804981] |
| HOP-62 | GI50 |
1.28 μM
Compound: 23, NSC-745885
|
Growth inhibition of human HOP62 cells
Growth inhibition of human HOP62 cells
|
[PMID: 19804981] |
| HOP-92 | GI50 |
2.52 μM
Compound: 23, NSC-745885
|
Growth inhibition of human HOP92 cells
Growth inhibition of human HOP92 cells
|
[PMID: 19804981] |
| Hs-578T | GI50 |
1.41 μM
Compound: 23, NSC-745885
|
Growth inhibition of human Hs 578T cells
Growth inhibition of human Hs 578T cells
|
[PMID: 19804981] |
| HT-29 | GI50 |
13.4 μM
Compound: 23, NSC-745885
|
Growth inhibition of human HT-29 cells
Growth inhibition of human HT-29 cells
|
[PMID: 19804981] |
| IGROV-1 | GI50 |
1.36 μM
Compound: 23, NSC-745885
|
Growth inhibition of human IGROV1 cells
Growth inhibition of human IGROV1 cells
|
[PMID: 19804981] |
| K562 | GI50 |
1.92 μM
Compound: 23, NSC-745885
|
Growth inhibition of human K562 cells
Growth inhibition of human K562 cells
|
[PMID: 19804981] |
| KM12 | GI50 |
1.96 μM
Compound: 23, NSC-745885
|
Growth inhibition of human KM12 cells
Growth inhibition of human KM12 cells
|
[PMID: 19804981] |
| LOX IMVI | GI50 |
0.82 μM
Compound: 23, NSC-745885
|
Growth inhibition of human LOXIMVI cells
Growth inhibition of human LOXIMVI cells
|
[PMID: 19804981] |
| M14 | GI50 |
2.15 μM
Compound: 23, NSC-745885
|
Growth inhibition of human M14 cells
Growth inhibition of human M14 cells
|
[PMID: 19804981] |
| Malme-3M | GI50 |
1.66 μM
Compound: 23, NSC-745885
|
Growth inhibition of human MALME-3M cells
Growth inhibition of human MALME-3M cells
|
[PMID: 19804981] |
| MCF7 | GI50 |
1.53 μM
Compound: 23, NSC-745885
|
Growth inhibition of human MCF7 cells
Growth inhibition of human MCF7 cells
|
[PMID: 19804981] |
| MDA-MB-231 | GI50 |
1.75 μM
Compound: 23, NSC-745885
|
Growth inhibition of human MDA-MB-231 cells
Growth inhibition of human MDA-MB-231 cells
|
[PMID: 19804981] |
| MDA-MB-435 | GI50 |
1.91 μM
Compound: 23, NSC-745885
|
Growth inhibition of human MDA-MB-435 cells
Growth inhibition of human MDA-MB-435 cells
|
[PMID: 19804981] |
| MOLT-4 | GI50 |
0.49 μM
Compound: 23, NSC-745885
|
Growth inhibition of human MOLT4 cells
Growth inhibition of human MOLT4 cells
|
[PMID: 19804981] |
| NCI/ADR-RES | GI50 |
1.86 μM
Compound: 23, NSC-745885
|
Growth inhibition of human NCI/ADR-RES cells
Growth inhibition of human NCI/ADR-RES cells
|
[PMID: 19804981] |
| NCI-H226 | GI50 |
4.48 μM
Compound: 23, NSC-745885
|
Growth inhibition of human NCI-H226 cells
Growth inhibition of human NCI-H226 cells
|
[PMID: 19804981] |
| NCI-H23 | GI50 |
1.44 μM
Compound: 23, NSC-745885
|
Growth inhibition of human NCI-H23 cells
Growth inhibition of human NCI-H23 cells
|
[PMID: 19804981] |
| NCI-H322M | GI50 |
17.4 μM
Compound: 23, NSC-745885
|
Growth inhibition of human NCI-H322M cells
Growth inhibition of human NCI-H322M cells
|
[PMID: 19804981] |
| NCI-H460 | GI50 |
3.27 μM
Compound: 23, NSC-745885
|
Growth inhibition of human NCI-H460 cells
Growth inhibition of human NCI-H460 cells
|
[PMID: 19804981] |
| NCI-H522 | GI50 |
1.66 μM
Compound: 23, NSC-745885
|
Growth inhibition of human NCI-H522 cells
Growth inhibition of human NCI-H522 cells
|
[PMID: 19804981] |
| OVCAR-3 | GI50 |
0.55 μM
Compound: 23, NSC-745885
|
Growth inhibition of human OVCAR-3 cells
Growth inhibition of human OVCAR-3 cells
|
[PMID: 19804981] |
| OVCAR-4 | GI50 |
0.65 μM
Compound: 23, NSC-745885
|
Growth inhibition of human OVCAR4 cells
Growth inhibition of human OVCAR4 cells
|
[PMID: 19804981] |
| OVCAR-5 | GI50 |
1.91 μM
Compound: 23, NSC-745885
|
Growth inhibition of human OVCAR5 cells
Growth inhibition of human OVCAR5 cells
|
[PMID: 19804981] |
| OVCAR-8 | GI50 |
1.66 μM
Compound: 23, NSC-745885
|
Growth inhibition of human OVCAR8 cells
Growth inhibition of human OVCAR8 cells
|
[PMID: 19804981] |
| PC-3 | GI50 |
3.23 μM
Compound: 23, NSC-745885
|
Growth inhibition of human PC3 cells
Growth inhibition of human PC3 cells
|
[PMID: 19804981] |
| PC-3 | IC50 |
2.5 μM
Compound: 2, NSC745885
|
Cytotoxicity against human PC3 cells after 48 hrs by SRB assay
Cytotoxicity against human PC3 cells after 48 hrs by SRB assay
|
[PMID: 26344783] |
| RXF 393 | GI50 |
1.75 μM
Compound: 23, NSC-745885
|
Growth inhibition of human RXF393 cells
Growth inhibition of human RXF393 cells
|
[PMID: 19804981] |
| SF-268 | GI50 |
2.17 μM
Compound: 23, NSC-745885
|
Growth inhibition of human SF268 cells
Growth inhibition of human SF268 cells
|
[PMID: 19804981] |
| SF-295 | GI50 |
1.9 μM
Compound: 23, NSC-745885
|
Growth inhibition of human SF295 cells
Growth inhibition of human SF295 cells
|
[PMID: 19804981] |
| SF-539 | GI50 |
1.46 μM
Compound: 23, NSC-745885
|
Growth inhibition of human SF539 cells
Growth inhibition of human SF539 cells
|
[PMID: 19804981] |
| SK-MEL-2 | GI50 |
1.68 μM
Compound: 23, NSC-745885
|
Growth inhibition of human SK-MEL-2 cells
Growth inhibition of human SK-MEL-2 cells
|
[PMID: 19804981] |
| SK-MEL-28 | GI50 |
1.85 μM
Compound: 23, NSC-745885
|
Growth inhibition of human SK-MEL-28 cells
Growth inhibition of human SK-MEL-28 cells
|
[PMID: 19804981] |
| SK-MEL-5 | GI50 |
1.58 μM
Compound: 23, NSC-745885
|
Growth inhibition of human SK-MEL-5 cells
Growth inhibition of human SK-MEL-5 cells
|
[PMID: 19804981] |
| SK-OV-3 | GI50 |
7.71 μM
Compound: 23, NSC-745885
|
Growth inhibition of human SKOV3 cells
Growth inhibition of human SKOV3 cells
|
[PMID: 19804981] |
| SN12C | GI50 |
1.33 μM
Compound: 23, NSC-745885
|
Growth inhibition of human SN12C cells
Growth inhibition of human SN12C cells
|
[PMID: 19804981] |
| SNB-19 | GI50 |
2.28 μM
Compound: 23, NSC-745885
|
Growth inhibition of human SNB19 cells
Growth inhibition of human SNB19 cells
|
[PMID: 19804981] |
| SNB-75 | GI50 |
2.03 μM
Compound: 23, NSC-745885
|
Growth inhibition of human SNB75 cells
Growth inhibition of human SNB75 cells
|
[PMID: 19804981] |
| SW-620 | GI50 |
1.79 μM
Compound: 23, NSC-745885
|
Growth inhibition of human SW620 cells
Growth inhibition of human SW620 cells
|
[PMID: 19804981] |
| T47D | GI50 |
1.39 μM
Compound: 23, NSC-745885
|
Growth inhibition of human T47D cells
Growth inhibition of human T47D cells
|
[PMID: 19804981] |
| TK-10 | GI50 |
2.85 μM
Compound: 23, NSC-745885
|
Growth inhibition of human TK10 cells
Growth inhibition of human TK10 cells
|
[PMID: 19804981] |
| U-251 | GI50 |
1.61 μM
Compound: 23, NSC-745885
|
Growth inhibition of human U251 cells
Growth inhibition of human U251 cells
|
[PMID: 19804981] |
| UACC-257 | GI50 |
1.74 μM
Compound: 23, NSC-745885
|
Growth inhibition of human UACC257 cells
Growth inhibition of human UACC257 cells
|
[PMID: 19804981] |
| UACC-62 | GI50 |
1.45 μM
Compound: 23, NSC-745885
|
Growth inhibition of human UACC62 cells
Growth inhibition of human UACC62 cells
|
[PMID: 19804981] |
| UO-31 | GI50 |
1.62 μM
Compound: 23, NSC-745885
|
Growth inhibition of human UO31 cells
Growth inhibition of human UO31 cells
|
[PMID: 19804981] |
In Vitro
NSC745885 (0.5-4 μM; 24, 48 or 72 hours) has a growth inhibitory or death-promoting effect on the SAS cells, it significantly decreases the densities of cultured cells when compared with untreated cells. The IC50 of NSC745885 is 0.85 μM after 72 hours’ treatment[1].NSC745885 (0.5-4 μM; 24 hours) increases annexin V positive cells in a dose-dependent manner, and the differences appears as a dose-dependent manner[1].NSC745885 (0.5-2 μM; 24 or 48 hours) decreases XIAP protein levels and increases protein levels both as a dose-dependent manner in SAS cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:SAS cells is obtained from a poorly differentiated human squamous cell carcinoma
-
Concentration:0.5 μM, 1 μM, 1.5 μM, 2 μM, 4 μM
-
Incubation Time:24, 48, or 72 hours
-
Result:Decreases SAS cells growth as a time and dose-dependent manner.
-
Cell Line:SAS cells is obtained from a poorly differentiated human squamous cell carcinoma
-
Concentration:0.5 μM, 1 μM, 1.5 μM, 2 μM, 4 μM
-
Incubation Time:24 hours
-
Result:Decreases SAS cells growth as a time and dose-dependent manner.
-
Cell Line:SAS cells is obtained from a poorly differentiated human squamous cell carcinoma
-
Concentration:0.5 μM, 1 μM, 1.5 μM, 2 μM
-
Incubation Time:24 or 48 hours
-
Result:Increased cleaved caspase-3 expression and decreased XIAP expression.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Eight-week-old NOD/SCID (NOD.CB17 Prkdcscid/J) mice[1]
-
Dosage:2 mg/kg
-
Administration:Intraperitoneal injection; 2 mg/kg; once daily; 10 days
-
Result:Inhibited engrafted tumors growth in vivo.
Chemical Information
-
CAS No. 4219-52-7
-
Appearance Solid
-
Masse moléculaire 266.27
-
Formule C14H6N2O2S
-
Color Light yellow to yellow
-
SMILES
O=C(C1=C(C2=O)C3=NSN=C3C=C1)C4=C2C=CC=C4
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : < 1 mg/mL (insoluble or slightly soluble)
* NSC745885 is usually formulated as a suspension.
Pureté et documentation
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Fiche technique (278 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Chen YW, et al.A novel compound NSC745885 exerts an anti-tumor effect on tongue cancer SAS cells in vitro and in vivo.PLoS One. 2014 Aug 15;9(8):e104703. [Content Brief]
[2]. Tang SH, et al. Pharmacologic down-regulation of EZH2 suppresses bladder cancer in vitro and in vivo.Oncotarget. 2014 Nov 15;5(21):10342-55. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)