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AC710 Mesylate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AC710 Mesylate图片
CAS NO:1351522-05-8
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
AC710 mesylate, the mesylate salt of AC710, is a potent, orally bioactive, and selective inhibitor of PDGFR (platelet-derived growth factor receptor) family kinase with Kd values of 0.6, 1.57, 1, 1.3, 1.0 nM for FLT3, CSF1R, KIT, PDGFRα and PDGFRβ, respectively. As a PDGFR inhibitor, AC710 has potential anticancer activity. Results from a mouse tumor xenograft, a collagen-induced arthritis model, and a 7 day rat in vivo tolerability study culminated in the selection of AC710 as a preclinical development candidate.
理化性质和储存条件
Molecular Weight (MW) 658.81
FormulaC32H46N6O7S
CAS No.1351522-05-8 (mesylate);
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 10 mM
Water: <1 mg/mL
Ethanol: N/A
Solubility (In vivo)O=C(C1=NC=C(OC2CC(C)(C)N(CC)C(C)(C)C2)C=C1)NC3=CC=C(NC(NC4=NOC(C(C)(C)C)=C4)=O)C=C3. CS(=O)(O)=O
SynonymsAC 710 Mesylate; AC710 Mesylate; AC-710 Mesylate.
实验参考方法
In Vitro

In vitro activity: AC710 is a potent, orally active, and selective inhibitor of PDGFR (platelet-derived growth factor receptor) family kinase with Kd values of 0.6, 1.57, 1, 1.3, 1.0 nM for FLT3, CSF1R, KIT, PDGFRα and PDGFRβ, respectively. As a PDGFR inhibitor, AC710 has potential anticancer activity. Results from a mouse tumor xenograft, a collagen-induced arthritis model, and a 7 day rat in vivo tolerability study culminated in the selection of AC710 as a preclinical development candidate.


Kinase Assay: AC710 is a potent, orally active, and selective inhibitor of PDGFR (platelet-derived growth factor receptor) family kinase with Kd values of 0.6, 1.57, 1, 1.3, 1.0 nM for FLT3, CSF1R, KIT, PDGFRα and PDGFRβ, respectively.

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
Animal model Athymic nude mice models with subcutaneous flank-tumor xenograft model using the MV4-11cell line
Formulation & Dosage 0.3, 3, and 30 mg/kg
References ACS Med Chem Lett. 2012 Sep 24;3(12):997-1002