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AC 710

Names

[ CAS No. ]:
1351522-04-7

[ Name ]:
AC 710

[Synonym ]:
5-[(1-Ethyl-2,2,6,6-tetramethyl-4-piperidinyl)oxy]-N-[4-({[5-(2-methyl-2-propanyl)-1,2-oxazol-3-yl]carbamoyl}amino)phenyl]-2-pyridinecarboxamide
2-Pyridinecarboxamide, N-[4-[[[[5-(1,1-dimethylethyl)-3-isoxazolyl]amino]carbonyl]amino]phenyl]-5-[(1-ethyl-2,2,6,6-tetramethyl-4-piperidinyl)oxy]-
AC710

Biological Activity

[Description]:

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.

[Related Catalog]:

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Kit
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> FLT3
Research Areas >> Cancer

[Target]

PDGFRα:1.3 nM (Kd)

PDGFRβ:1 nM (Kd)

c-Kit:1 nM (Kd)

FLT3:0.6 nM (Kd)

CSF1R:1.57 nM (Kd)


[In Vivo]

At 0.3 mg/kg of AC710, tumor growth is temporally inhibited, and growth resumes quickly thereafter. At 3 and 30 mg/kg of AC710, tumors regress completely, and the tumor volume stays suppressed for an extended period after dosing is halted. No body weight loss is observed in animals treated with AC710 at all doses, indicating that it is well tolerated in mice at efficacious doses. AC710 exhibits a significant impact on disease in a dose-dependent fashion in a mouse collagen-induced arthritis (CIA) model, at a dose as low as 3 mg/ kg for 15 days (day 0-14). At 10 and 30 mg/kg, AC710 demonstrates equivalent or slightly better efficacy in reducing the joint swelling and inflammation than dexomethasone administered at a safe dose. AC710 is well tolerated at the tested doses[1].

[Animal admin]

Mice: The antitumor efficacy of AC710 is assessed in a subcutaneous flank-tumor xenograft model in athymic nude mice using the MV4-11cell line. AC710 is dosed at 0.3, 3, and 30 mg/kg for 2 weeks. Tumor growth and body weight is monitored[1].

[References]

[1]. Liu G, et al. 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.


[Related Small Molecules]

Pexidartinib | Nintedanib (BIBF 1120) | Gilteritinib | Quizartinib (AC220) | Crenolanib | Pacritinib | SU 5402 | Linifanib (ABT-869) | Cediranib | Masitinib (AB1010) | LY2784544 | DCC-2036 (Rebastinib) | SU14813 | Dovitinib (TKI-258, CHIR-258) | SB1317

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
580.4±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C31H42N6O4

[ Molecular Weight ]:
562.703

[ Flash Point ]:
304.8±30.1 °C

[ Exact Mass ]:
562.326782

[ PSA ]:
121.62000

[ LogP ]:
4.86

[ Vapour Pressure ]:
0.0±1.6 mmHg at 25°C

[ Index of Refraction ]:
1.591

[ Storage condition ]:
2-8℃


Related Compounds