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| 5mg |
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| 10mg |
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| 25mg |
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Purity: ≥98%
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.Because it inhibits PDGFR, AC710 may have anticancer properties. The preclinical development candidate for AC710 was chosen based on the outcomes of a seven-day in vivo tolerability study, a collagen-induced arthritis model, and a mouse tumor xenograft.
| Targets |
PDGFRα (Kd = 1.3 nM); PDGFRβ (Kd = 1 nM); c-Kit (Kd = 1 nM); FLT3 (Kd = 0.6 nM); CSF1R (Kd = 1.57 nM)
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| ln Vitro |
AC710 is a potent, orally active, and selective inhibits the PDGFR (platelet-derived growth factor receptor) family kinase, with Kd values of 0.6, 1.57, 1, 1.3, and 1.0 nM for FLT3, CSF1R, KIT, PDGFRα, and PDGFRβ, individually. AC710 may have anticancer properties because it is a PDGFR inhibitor. The preclinical development candidate AC710 was chosen based on outcomes from a rat in vivo tolerability study, a mouse tumor xenograft, and a collagen-induced arthritis model.
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| ln Vivo |
AC710 shows a dose-dependent effect on disease in a mouse model of collagen-induced arthritis (CIA), starting at a dose of 3 mg/kg and lasting for 15 days (days 0–14). When given at a safe dosage, dexomethasone reduces joint swelling and inflammation more effectively than AC710, either equally or marginally better. At the tested doses, AC710 is well tolerated[1]. Tumor growth is momentarily stopped at 0.3 mg/kg of AC710, but it soon resumes. Tumors fully regress at 3 and 30 mg/kg of AC710, and the tumor volume remains suppressed long after dosing is stopped. Animals treated with AC710 at all doses show no signs of body weight loss, suggesting that mice can tolerate it well at effective dosages.
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| Enzyme Assay |
AC710 is a potent, orally active, and selective inhibits the PDGFR (platelet-derived growth factor receptor) family kinase, with Kd values of 0.6, 1.57, 1, 1.3, and 1.0 nM for FLT3, CSF1R, KIT, PDGFRα, and PDGFRβ, individually.
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| Animal Protocol |
Mice: In athymic nude mice, the antitumor efficacy of AC710 is evaluated using the MV4-11cell line in a subcutaneous flank-tumor xenograft model. Over the course of two weeks, AC710 is dosed at0.3,3, and 30 mg/kg. Both body weight and tumor growth are tracked.
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| References |
| Molecular Formula |
C31H42N6O4
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|---|---|---|
| Molecular Weight |
562.7
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| Exact Mass |
562.326
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| Elemental Analysis |
C, 66.17; H, 7.52; N, 14.94; O, 11.37
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| CAS # |
1351522-04-7
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| Related CAS # |
AC710 Mesylate;1351522-05-8
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| PubChem CID |
54760053
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
580.4±50.0 °C at 760 mmHg
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| Flash Point |
304.8±30.1 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.591
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| LogP |
4.86
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
41
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| Complexity |
880
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(C1=C([H])N=C(C(N([H])C2C([H])=C([H])C(=C([H])C=2[H])N([H])C(N([H])C2C([H])=C(C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H])ON=2)=O)=O)C([H])=C1[H])C1([H])C([H])([H])C(C([H])([H])[H])(C([H])([H])[H])N(C([H])([H])C([H])([H])[H])C(C([H])([H])[H])(C([H])([H])[H])C1([H])[H]
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| InChi Key |
JVCWPUFNLFSKFS-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
N-[4-[(5-tert-butyl-1,2-oxazol-3-yl)carbamoylamino]phenyl]-5-(1-ethyl-2,2,6,6-tetramethylpiperidin-4-yl)oxypyridine-2-carboxamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.5 mg/mL (0.89 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.5 mg/mL (0.89 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.5 mg/mL (0.89 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 In vivo efficacy of compound22b (AC710)in mouse models.ACS Med Chem Lett.2012 Sep 24;3(12):997-1002. |
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ACS Med Chem Lett.2012 Sep 24;3(12):997-1002. |
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