WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406202
CAS#: 1351522-04-7 (free base)
Description: AC710 is a potent, orally active, and selective platelet-derived growth factor receptor-family kinase inhibitor with potential anticancer activity. Its IC50 values are 1.2, 2, 7.7 and 10.5 nM for KIT, FLT3, PDGFRβ and CSF1R respectively; Kd = 1.3 nM for PDGFRα.. AC710 causes tumor regression of leukemia cell xenografts in mice. AC710 also reduces joint swelling and inflammation in a mouse model of collagen-induced arthritis. AC710 is now a preclinical development candidate.
MedKoo Cat#: 406202
Name: AC710
CAS#: 1351522-04-7 (free base)
Chemical Formula: C31H42N6O4
Exact Mass: 562.32675
Molecular Weight: 562.7
Elemental Analysis: C, 66.17; H, 7.52; N, 14.94; O, 11.37
Related CAS #: 1351522-04-7 (free base) 1351522-05-8 (mesylate)
Synonym: AC710; AC 710; AC-710.
IUPAC/Chemical Name: N-(4-(3-(5-(tert-butyl)isoxazol-3-yl)ureido)phenyl)-5-((1-ethyl-2,2,6,6-tetramethylpiperidin-4-yl)oxy)picolinamide
InChi Key: JVCWPUFNLFSKFS-UHFFFAOYSA-N
InChi Code: InChI=1S/C31H42N6O4/c1-9-37-30(5,6)17-23(18-31(37,7)8)40-22-14-15-24(32-19-22)27(38)33-20-10-12-21(13-11-20)34-28(39)35-26-16-25(41-36-26)29(2,3)4/h10-16,19,23H,9,17-18H2,1-8H3,(H,33,38)(H2,34,35,36,39)
SMILES Code: O=C(NC1=CC=C(NC(NC2=NOC(C(C)(C)C)=C2)=O)C=C1)C3=NC=C(OC4CC(C)(C)N(CC)C(C)(C)C4)C=C3
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: >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: | AC710 is a potent PDGFR inhibitor with Kds of 0.6, 1.57, 1, 1.3, 1.0 nM for FLT3, CSF1R, KIT, PDGFRα and PDGFRβ, respectively. |
| In vitro activity: | TBD |
| In vivo activity: | TBD |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 13.0 | 23.1 |
The following data is based on the product molecular weight 562.7 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 |
| In vitro protocol: | TBD |
| In vivo protocol: | TBD |
1: Liu G, Campbell BT, Holladay MW, Ford Pulido JM, Hua H, Gitnick D, Gardner MF, James J, Breider MA, Brigham D, Belli B, Armstrong RC, Treiber DK. Discovery of AC710, a Globally Selective Inhibitor of Platelet-Derived Growth Factor Receptor-Family Kinases. ACS Med Chem Lett. 2012 Sep 24;3(12):997-1002. doi: 10.1021/ml300214g. PMID: 24900421; PMCID: PMC4025831.
2: Díaz-Lezama N, Wolf A, Koch S, Pfaller AM, Biber J, Guillonneau X, Langmann T, Grosche A. PDGF Receptor Alpha Signaling Is Key for Müller Cell Homeostasis Functions. Int J Mol Sci. 2021 Jan 25;22(3):1174. doi: 10.3390/ijms22031174. PMID: 33503976; PMCID: PMC7865899.
