Synonym
Cyclin-dependent kinase 1/5 Inhibitor; Cdk1/5 Inhibitor; NSC 693868; NSC693868; NSC-693868
IUPAC/Chemical Name
1H-pyrazolo[3,4-b]quinoxalin-3-amine
InChi Key
DWHVZCLBMTZRQM-UHFFFAOYSA-N
InChi Code
InChI=1S/C9H7N5/c10-8-7-9(14-13-8)12-6-4-2-1-3-5(6)11-7/h1-4H,(H3,10,12,13,14)
SMILES Code
NC1=NNC2=NC3=C(N=C21)C=CC=C3
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
Biological target:
NSC693868 is a selective inhibitor of CDK1 and CDK5 with IC50s of 600 nM and 400 nM.
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMF |
3.0 |
16.20 |
| DMSO |
5.0 |
27.00 |
| DMSO:PBS (pH 7.2) (1:1) |
0.5 |
2.70 |
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
185.19
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. Bettayeb, K., Baunbaek, D., Delehouze, C., et al. CDK inhibitors roscovitine and CR8 trigger Mcl-I down-regulation and apoptotic cell death in neuroblastoma cells. Genes Cancer 1(4), 369-380 (2010).
2. Ortega, M.A., Montoya, M.E., Zarranz, B., et al. Pyrazolo[3,4-b]quinoxalines. A new class of cyclin-dependent kinases inhibitors. Bioorganic & Medicinal Chemistry 10(7), 2177-2184 (2002).
3. Chen, S., Xu, Y., Yuan, X., et al. Androgen receptor phosphorylation and stabilization in prostate cancer by cyclin-dependent kinase 1. Proceedings of the National Academy of Sciences of the United States of America 103(43), 15969-15974 (2006).
4. Nguyen, T.K., and Grant, S. Dinaciclib (SCH727965) inhibits the unfolded protein response through a CDK1- and 5-dependent mechanism. Molecular Cancer Therapeutics 13(3), 662-674 (2014).
5. Topanurak, S., Ferraris, J.D., Li, J., et al. High NaCl- and urea-induced posttranslational modifications that increase glycerophosphocholine by inhibiting GDPD5 phosphodiesterase. Proceedings of the National Academy of Sciences of the United States of America 110(18), 7482-7487 (2013).
