Synonym
8-Nitrotryptanthrin; GNF-PF-3777
IUPAC/Chemical Name
8-nitro-indolo[2,1-b]quinazoline-6,12-dione
InChi Key
UFMQJYHLIUACCG-UHFFFAOYSA-N
InChi Code
InChI=1S/C15H7N3O4/c19-13-10-7-8(18(21)22)5-6-12(10)17-14(13)16-11-4-2-1-3-9(11)15(17)20/h1-7H
SMILES Code
O=C1C2=CC=CC=C2N=C3N1C(C=CC([N+]([O-])=O)=C4)=C4C3=O
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
>3 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
More Info
λmax: 229, 262, 322, 382 nm
Biological target:
GNF-PF-3777 (8-Nitrotryptanthrin) is a potent human indoleamine 2,3-dioxygenase 2 (hIDO2) inhibitor which significantly reduces IDO2 activity with Ki of 0.97 μM.
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMSO |
4.2 |
14.32 |
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
293.24
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:
TBD
1. Yang, S., Li, X., Hu, F., et al. Discovery of tryptanthrin derivatives as potent inhibitors of indoleamine 2,3-dioxygenase with therapeutic activity in Lewis lung cancer (LLC) tumor-bearing mice. J. Med. Chem. 56(21), 8321-8331 (2013).
2. Sharma, V.M., Prasanna, P., Seshu, K.V., et al. Novel indolo[2,1-b]quinazoline analogues as cytostatic agents: Synthesis, biological evaluation and structure-activity relationship. Bioorg. Med. Chem. Lett. 12(17), 2303-2307 (2002).
3. Hwang, J.-M., Oh, T., Kaneko, T., et al. Design, synthesis, and structure-activity relationship studies of tryptanthrins as antitubercular agents. J. Nat. Prod. 76(3), 354-367 (2013).
4. Kawakami, J., Matsushima, N., Ogawa, O., et al. Antibacterial and antifungal activities of tryptanthrin derivatives. Trans. Mater. Res. Soc. Jpn. 36(4), 603-606 (2011).
5. Scovill, J., Blank, E., Konnick, M., et al. Antitrypanosomal activities of tryptanthrins. Antimicrob. Agents Chemother. 46(3), 882-883 (2002).
