Synonym
AG 12286; AG-12286; AG12286; AG 012286; AG-012286; AG012286;AG-012986 analog; AG012986 analog; AG 012986 analog;
IUPAC/Chemical Name
Benzenesulfonamide, 4-((4-amino-5-(2,6-difluorobenzoyl)-2-thiazolyl)amino)-
InChi Key
BWWQFAUYHCRZKB-UHFFFAOYSA-N
InChi Code
1S/C16H12F2N4O3S2/c17-10-2-1-3-11(18)12(10)13(23)14-15(19)22-16(26-14)21-8-4-6-9(7-5-8)27(20,24)25/h1-7H,19H2,(H,21,22)(H2,20,24,25)
SMILES Code
O=S(C1=CC=C(NC2=NC(N)=C(C(C3=C(F)C=CC=C3F)=O)S2)C=C1)(N)=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
Preparing Stock Solutions
The following data is based on the
product
molecular weight
410.41
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 |
1: Huang W, Collette W 3rd, Twamley M, Aguirre SA, Sacaan A. Application of electroretinography (ERG) in early drug development for assessing retinal toxicity in rats. Toxicol Appl Pharmacol. 2015 Dec 15;289(3):525-33. doi: 10.1016/j.taap.2015.10.008. Epub 2015 Oct 19. PubMed PMID: 26482841.
2: Lee DU, Jessen B. Off-target immune cell toxicity caused by AG-012986, a pan-CDK inhibitor, is associated with inhibition of p38 MAPK phosphorylation. J Biochem Mol Toxicol. 2012 Mar;26(3):101-8. doi: 10.1002/jbt.20415. Epub 2011 Nov 16. PubMed PMID: 22095879.
3: Zhang C, Lundgren K, Yan Z, Arango ME, Price S, Huber A, Higgins J, Troche G, Skaptason J, Koudriakova T, Nonomiya J, Yang M, O'Connor P, Bender S, Los G, Lewis C, Jessen B. Pharmacologic properties of AG-012986, a pan-cyclin-dependent kinase inhibitor with antitumor efficacy. Mol Cancer Ther. 2008 Apr;7(4):818-28. doi: 10.1158/1535-7163.MCT-07-0440. PubMed PMID: 18413795.
4: Jessen BA, Lee L, Koudriakova T, Haines M, Lundgren K, Price S, Nonomiya J, Lewis C, Stevens GJ. Peripheral white blood cell toxicity induced by broad spectrum cyclin-dependent kinase inhibitors. J Appl Toxicol. 2007 Mar-Apr;27(2):133-42. PubMed PMID: 17211896.
5: Illanes O, Anderson S, Niesman M, Zwick L, Jessen BA. Retinal and peripheral nerve toxicity induced by the administration of a pan-cyclin dependent kinase (cdk) inhibitor in mice. Toxicol Pathol. 2006;34(3):243-8. PubMed PMID: 16698721.
