AG-012986

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406184

CAS#: 486414-35-1 (free base)

Description: AG-012986 is a multitargeted cyclin-dependent kinase (CDK) inhibitor active against CDK1, CDK2, CDK4/6, CDK5, and CDK9, with selectivity over a diverse panel of non-CDK kinases. AG-012986 showed antiproliferative activities in vitro with IC(50)s of <100 nmol/L in 14 of 18 tumor cell lines. In vivo, significant antitumor efficacy induced by AG-012986 was seen (tumor growth inhibition, >83.1%) in 10 of 11 human xenograft tumor models. AG-012986 also showed dose-dependent retinoblastoma Ser(795) hypophosphorylation, cell cycle arrest, decreased Ki-67 tumor staining, and apoptosis in conjunction with antitumor activity. Note: many vendors confused the structure of AG-12286 (CAT#573461, CAS# 223784-75-6) with AG-012986 (CAT#406184, CAS# is 486414-35-1).


Chemical Structure

img
AG-012986
CAS# 486414-35-1 (free base)

Theoretical Analysis

MedKoo Cat#: 406184
Name: AG-012986
CAS#: 486414-35-1 (free base)
Chemical Formula: C22H23F2N5O2S
Exact Mass: 459.15405
Molecular Weight: 459.51
Elemental Analysis: C, 57.50; H, 5.05; F, 8.27; N, 15.24; O, 6.96; S, 6.98

Size Price Shipping out time Quantity
Inquire bulk and customized quantity

Pricing updated 2021-03-08. Prices are subject to change without notice.

AG-012986, purity > 98%, is not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.

Related CAS #: 223784-75-6   486414-35-1 (free base)   486414-32-8 (HCl)    

Synonym: AG012986; AG 012986; AG-012986; AG12986; AG 12986; AG-12986.

IUPAC/Chemical Name: 4-[[4-Amino-5-(2,6-difluorobenzoyl)thiazol-2-yl]amino]-N-((R)-2-dimethylamino-1-methylethyl)benzamide

InChi Key: KFWFBALDPSVAFT-GFCCVEGCSA-N

InChi Code: InChI=1S/C22H23F2N5O2S/c1-12(11-29(2)3)26-21(31)13-7-9-14(10-8-13)27-22-28-20(25)19(32-22)18(30)17-15(23)5-4-6-16(17)24/h4-10,12H,11,25H2,1-3H3,(H,26,31)(H,27,28)/t12-/m1/s1

SMILES Code: O=C(N[C@H](C)CN(C)C)C1=CC=C(NC2=NC(N)=C(C(C3=C(F)C=CC=C3F)=O)S2)C=C1

Appearance:
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, not in water

Shelf Life:
>5 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

Handling Instructions:

Preparing Stock Solutions

The following data is based on the product molecular weight 459.51 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.

Select a batch to recalculate based on the batch molecular weight:
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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

1: 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.

2: 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.

3: 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.

4: 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.



Additional Information