Art. -Nr.: HY-107194

NSC12

NSC12 is an orally active pan-FGF trap. NSC12 inhibits the interaction between FGF2/FGFR. NSC12 suppresses the phosphorylation of FGFR3. NSC12 reduces c-Myc levels, induces DNA damage, triggers the cleavage of Caspase 3, and promotes ROS production. NSC12 exhibits anticancer activity against lung cancer and multiple myeloma.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 102586-30-1
Formel: C₂₄H₃₄F₆O₃
Molecular Weight:484.52

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

NSC12 Chemical Structure

CAS. Nr.: 102586-30-1

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

Caspase 3

FGFR3

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen :

Alle Caspase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	IC₅₀	10 μM Compound: 11	Inhibition of human recombinant FGF2 assessed as reduction in HSPG/FGF2/FGDR interaction by measuring FGF2 mediated A475-CHO-flg-1A-luc cell to CHO-K1 cell adhesion incubated for 2 hrs by luciferase assay Inhibition of human recombinant FGF2 assessed as reduction in HSPG/FGF2/FGDR interaction by measuring FGF2 mediated A475-CHO-flg-1A-luc cell to CHO-K1 cell adhesion incubated for 2 hrs by luciferase assay	[PMID: 27138345]
KMS-11	IC₅₀	3.4 μM Compound: 1; NSC12	Antiproliferative activity against human KMS-11 cells assessed as reduction in cell viability incubated for 48 hrs by propidium iodide staining-based flow cytometric analysis Antiproliferative activity against human KMS-11 cells assessed as reduction in cell viability incubated for 48 hrs by propidium iodide staining-based flow cytometric analysis	[PMID: 34004471]
Lewis lung carcinoma cell line	IC₅₀	2 μM Compound: 11	Antiproliferative activity against mouse LLC cells incubated for 48 hrs by PI-staining based flow cytometry Antiproliferative activity against mouse LLC cells incubated for 48 hrs by PI-staining based flow cytometry	[PMID: 27138345]
NCI-H520	IC₅₀	4.1 μM Compound: 11	Antiproliferative activity against human NCI-H520 cells incubated for 72 hrs by PI-staining based flow cytometry Antiproliferative activity against human NCI-H520 cells incubated for 72 hrs by PI-staining based flow cytometry	[PMID: 27138345]

In Vitro

NSC12 (0.3-10.0 μM; 48 h for LLC cells, 72 h for H520 cells) inhibits the proliferation of mouse Lewis lung carcinoma (LLC) cells and H520 lung cancer cells, with an IC₅₀ of 2.0 μM for the former and 4.1 μM for the latter^[1].
NSC12 (6 μM; 6 h) inhibits FGFR3 phosphorylation by 75% in multiple myeloma KMS-11 cells treated with 6 μM NSC12 for 6 h^[2].
NSC12 (6 μM; 6 h) inhibits FGFR phosphorylation in multiple myeloma cell lines KMS-11, OPM-2, U-266, and the Bortezomib-resistant strain KMS-11/BTZ^[2].
NSC12 (6 μM; 6 h) reduces c-Myc levels and induces DNA damage in multiple myeloma KMS-11 cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:

murine Lewis lung carcinoma (LLC) cells, human H520 lung carcinoma cells
Concentration:

0.3-10.0 μM
Incubation Time:

48 h (LLC cells); 72 h (H520 cells)
Result:

Efficiently impaired proliferation of both FGF-dependent cell lines, with an IC₅₀ of 2.0 μM for LLC cells and 4.1 μM for H520 cells.

Western Blot Analysis^[2]

Cell Line:

human multiple myeloma KMS-11 cells (t(4;14) translocation, FGFR3 overexpression)
Concentration:

6 μM
Incubation Time:

6 h
Result:

Inhibited FGFR3 phosphorylation by 75%.

Cell Viability Assay^[2]

Cell Line:

human multiple myeloma cell lines KMS-11, OPM-2, U-266, and bortezomib-resistant KMS-11/BTZ
Concentration:

0.1-10.0 μM
Incubation Time:

48 h
Result:

Inhibited cell viability with the following half-maximal inhibitory concentrations (IC₅₀): 3.6 μM (KMS-11), 4.4 μM (OPM-2), 3.4 μM (U-266), 3.6 μM (KMS-11/BTZ).

Western Blot Analysis^[2]

Cell Line:

human multiple myeloma KMS-11 cells
Concentration:

6 μM
Incubation Time:

6 h
Result:

Strongly reduced c-Myc protein levels.
Increased γH2AX (DNA damage marker) levels.
Induced cleavage of caspase 3 (apoptosis marker).

In Vivo

NSC12 (7.5 mg/kg; i.p.; every other day) reduces multiple myeloma tumor growth by ~40% in NOD/SCID mice, inhibits FGFR signaling, and induces tumor cell death without causing measurable toxicity^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

NOD/SCID (female, 6-8-week-old)^[2]
Dosage:

7.5 mg/kg
Administration:

i.p.; every other day
Result:

Reduced tumor growth by approximately 40% compared to vehicle control.
Lowered tumor weight significantly compared to vehicle control.
Inhibited tumor FGFR phosphorylation.
Reduced c-Myc protein levels.
Increased tissue oxidative stress (nitrotyrosine staining).
Increased DNA damage (γH2AX staining).
Reduced tumor cell proliferation (pHH3 staining).
Increased apoptotic cell death (cleaved caspase 3 staining).
Caused no significant changes in mouse body weight, blood cell composition, blood biochemical parameters, or blood phosphorus/calcium levels.

Chemical Information

CAS. Nr. 102586-30-1
Appearance Solid
Molecular Weight 484.52
Formel C₂₄H₃₄F₆O₃
Color White to light yellow
SMILES

C[C@@]12[C@](CC[C@]2([H])[C@@H](O)CC(C(F)(F)F)(O)C(F)(F)F)([H])[C@@]3([H])[C@@](CC1)([H])[C@@]4(C(C[C@H](CC4)O)=CC3)C
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 10 mg/mL (20.64 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0639 mL

10.3195 mL

20.6390 mL

5 mM

0.4128 mL

2.0639 mL

4.1278 mL

10 mM

0.2064 mL

1.0319 mL

2.0639 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (536 KB)
- English - EN (536 KB)
- Français - FR (536 KB)
- Deutsch - DE (536 KB)
- Norwegian - NO (536 KB)
- Español - ES (536 KB)
- Swedish - SV (536 KB)
- Italian - IT (536 KB)
- Korean - KR (536 KB)
- Portuguese - PT (536 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Castelli R, et al. Synthesis, Structural Elucidation, and Biological Evaluation of NSC12, an Orally Available Fibroblast Growth Factor (FGF) Ligand Trap for the Treatment of FGF-Dependent Lung Tumors. J Med Chem. 2016;59(10):4651-4663. [Content Brief]

[2]. Taranto S, et al. Discovery of novel FGF trap small molecules endowed with anti-myeloma activity. Pharmacol Res. 2024;206:107291. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0639 mL	10.3195 mL	20.6390 mL	51.5975 mL
	5 mM	0.4128 mL	2.0639 mL	4.1278 mL	10.3195 mL
	10 mM	0.2064 mL	1.0319 mL	2.0639 mL	5.1597 mL
	15 mM	0.1376 mL	0.6880 mL	1.3759 mL	3.4398 mL
	20 mM	0.1032 mL	0.5160 mL	1.0319 mL	2.5799 mL

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

NSC12

High-Throughput Bioactive Compound Library

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Alle Caspase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

NSC12 Related Classifications

HY-107194 Related Classifications