[CAS NO. 1351522-04-7]  AC710

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PRODUCTS SPECIFICATIONS [1351522-04-7]

Catalog
HY-13493
Brand
MCE
CAS
1351522-04-7

DESCRIPTION [1351522-04-7]

Overview

MDLMFCD25976599
Molecular Weight562.70
Molecular FormulaC31H42N6O4
SMILESO=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

For research use only. We do not sell to patients.

Summary

AC710 is a potent PDGFR inhibitor with K d s of 0.6, 1.57, 1, 1.3, 1.0 nM for FLT3 , CSF1R, KIT, PDGFRα and PDGFRβ , respectively.


IC50 & 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] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : 14 mg/mL ( 24.88 mM ; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7771 mL 8.8857 mL 17.7715 mL
5 mM 0.3554 mL 1.7771 mL 3.5543 mL
10 mM 0.1777 mL 0.8886 mL 1.7771 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 0.5 mg/mL (0.89 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 0.5 mg/mL (0.89 mM); Clear solution

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 0.5 mg/mL (0.89 mM); Clear solution

* All of the co-solvents are available by MCE.