Synonym
SU-4312; SU 4312; SU4312. DMBI; NSC 86429; NSC-86429; NSC86429.
IUPAC/Chemical Name
3-[[4-(dimethylamino)phenyl]methylene]-1,3-dihydro-2H-indol-2-one
InChi Key
UAKWLVYMKBWHMX-PTNGSMBKSA-N
InChi Code
UAKWLVYMKBWHMX-PTNGSMBKSA-N
SMILES Code
O=C1NC2=C(C=CC=C2)/C1=C/C3=CC=C(N(C)C)C=C3
Appearance
Yellow solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
SU-4312 is an inhibitor of VEGFR2 and PDGFR tyrosine kinases (IC50s = 0.8 and 19.4 μM, respectively). It demonstrates IC50 values >100 μM at EGFR, HER2, and IGF-1R. SU-4312 has been shown to inhibit VEGF-dependent angiogenesis in a zebrafish assay (IC50 = 1.8 µM) without affecting normal cells.
In vitro activity:
To be determined
In vivo activity:
In a murine model of Parkinson’s disease (PD), SU4312 administration improved motor function, restored MEF2D levels, and inhibited oxidative stress. It also preserved dopaminergic neurons, mitochondrial biogenesis, and inhibited MAO-B activity. These results suggest SU4312 as a promising candidate for PD treatment, acting through multiple mechanisms.
Reference: Neuropharmacology. 2017 Nov;126:12-24. https://pubmed.ncbi.nlm.nih.gov/28807675/
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMF |
30.0 |
113.49 |
| DMF:PBS (pH 7.2) (1:2) |
0.3 |
1.13 |
| DMSO |
10.0 |
37.83 |
| Ethanol |
0.3 |
0.95 |
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
264.33
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
1. Guo B, Hu S, Zheng C, Wang H, Luo F, Li H, Cui W, Yang X, Cui G, Mak S, Choi TC, Ma ED, Wang Y, Lee SMY, Zhang Z, Han Y. Substantial protection against MPTP-associated Parkinson's neurotoxicity in vitro and in vivo by anti-cancer agent SU4312 via activation of MEF2D and inhibition of MAO-B. Neuropharmacology. 2017 Nov;126:12-24. doi: 10.1016/j.neuropharm.2017.08.014. Epub 2017 Aug 12. PMID: 28807675.
2. Cui W, Zhang Z, Li W, Hu S, Mak S, Zhang H, Han R, Yuan S, Li S, Sa F, Xu D, Lin Z, Zuo Z, Rong J, Ma ED, Choi TC, Lee SM, Han Y. The anti-cancer agent SU4312 unexpectedly protects against MPP(+) -induced neurotoxicity via selective and direct inhibition of neuronal NOS. Br J Pharmacol. 2013 Mar;168(5):1201-14. doi: 10.1111/bph.12004. PMID: 23062100; PMCID: PMC3594677.
In vitro protocol:
To be determined
In vivo protocol:
1. Guo B, Hu S, Zheng C, Wang H, Luo F, Li H, Cui W, Yang X, Cui G, Mak S, Choi TC, Ma ED, Wang Y, Lee SMY, Zhang Z, Han Y. Substantial protection against MPTP-associated Parkinson's neurotoxicity in vitro and in vivo by anti-cancer agent SU4312 via activation of MEF2D and inhibition of MAO-B. Neuropharmacology. 2017 Nov;126:12-24. doi: 10.1016/j.neuropharm.2017.08.014. Epub 2017 Aug 12. PMID: 28807675.
2. Cui W, Zhang Z, Li W, Hu S, Mak S, Zhang H, Han R, Yuan S, Li S, Sa F, Xu D, Lin Z, Zuo Z, Rong J, Ma ED, Choi TC, Lee SM, Han Y. The anti-cancer agent SU4312 unexpectedly protects against MPP(+) -induced neurotoxicity via selective and direct inhibition of neuronal NOS. Br J Pharmacol. 2013 Mar;168(5):1201-14. doi: 10.1111/bph.12004. PMID: 23062100; PMCID: PMC3594677.
1: Li Y, Zhu H, Klausen C, Peng B, Leung PC. Vascular Endothelial Growth Factor-A
(VEGF-A) Mediates Activin A-Induced Human Trophoblast Endothelial-Like Tube
Formation. Endocrinology. 2015 Nov;156(11):4257-68. doi: 10.1210/en.2015-1228.
PubMed PMID: 26327470.
2: Cui W, Zhang Z, Li W, Hu S, Mak S, Zhang H, Han R, Yuan S, Li S, Sa F, Xu D,
Lin Z, Zuo Z, Rong J, Ma ED, Choi TC, Lee SM, Han Y. The anti-cancer agent SU4312
unexpectedly protects against MPP(+) -induced neurotoxicity via selective and
direct inhibition of neuronal NOS. Br J Pharmacol. 2013 Mar;168(5):1201-14. doi:
10.1111/bph.12004. PubMed PMID: 23062100; PubMed Central PMCID: PMC3594677.
3: Miki A, Miki K, Ueno S, Wersinger DM, Berlinicke C, Shaw GC, Usui S, Wang Y,
Zack DJ, Campochiaro PA. Prolonged blockade of VEGF receptors does not damage
retinal photoreceptors or ganglion cells. J Cell Physiol. 2010 Jul;224(1):262-72.
doi: 10.1002/jcp.22129. PubMed PMID: 20232317; PubMed Central PMCID: PMC4005719.
4: Schultheiss C, Blechert B, Gaertner FC, Drecoll E, Mueller J, Weber GF,
Drzezga A, Essler M. In vivo characterization of endothelial cell activation in a
transgenic mouse model of Alzheimer's disease. Angiogenesis. 2006;9(2):59-65.
PubMed PMID: 16821113.
