2. Protein Tyrosine Kinase/RTK Apoptosis Cell Cycle/DNA Damage Immunology/Inflammation NF-κB Metabolic Enzyme/Protease
  3. FGFR c-Myc DNA/RNA Synthesis Caspase Reactive Oxygen Species (ROS)
  4. 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.

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NSC12

NSC12 Chemical Structure

CAS No. : 102586-30-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

NSC12 Related Antibodies

Top Publications Citing Use of Products

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RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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Description

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[1][2].

IC50 & Target[1]

Caspase 3

 

FGFR3

 

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]
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.

NSC12 Related Antibodies

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.
Molecular Weight

484.52

Formula

C24H34F6O3
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0639 mL 10.3195 mL 20.6390 mL
5 mM 0.4128 mL 2.0639 mL 4.1278 mL
View the Complete Stock Solution Preparation Table

* 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.

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Purity & Documentation

Purity: 99.27%

SDS (536 KB)

COA (250 KB) HNMR (139 KB) RP-HPLC (272 KB) MS (71 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* 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.

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
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NSC12 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NSC12102586-30-1NSC 12NSC-12FGFRc-MycDNA/RNA SynthesisCaspaseReactive Oxygen Species (ROS)Fibroblast growth factor receptorMycLewis lung carcinoma (LLC) cellsKMS-11 cellsHSPG/FGF/FGFR ternary complexCHO-K1 cellsA745-CHO-flg-1A-luc cellsOPM-2 cellsH520 lung carcinoma cellsFGF2U-266 cellsInhibitorinhibitorinhibit

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