| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
AZD7507 is a novel, potent, selective and orally bioactive 3-amido-4-anilinoquinoline CSF-1R inhibitor with 32 nM cell activity and with antitumor activity. Given that it maintained AZ683's oral pharmacokinetic characteristics and intended potency, AZD7507 is regarded as a promising compound. Furthermore, no changes were observed in the ECG, no rise in troponin associated with the treatment, and no cardiovascular toxicity was observed in dogs receiving a single oral dosage in a telemetry study.
| Targets |
CSF-1R
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|---|---|
| ln Vitro |
AZD7507 (Compound 31) exhibits inhibitory activity against hERG and NaV1.5, with IC50s of >30 and 26 μM, respectively. It also inhibits the proliferation of 3T3 cells that have been engineered to express CSF-1R and stimulated with CSF-1 (IC50, 32 nM)[1].
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| ln Vivo |
AZD7507 exhibits a good oral PK in rats, with a 42% bioavailability and an in vivo clearance of 7 mL/min/kg. The IC50 in the canine L-type Ca channel assay is greater than 20 μM[1]. Mice bearing CC-LP-1 and SNU-1079 cells exhibit a significant reduction in volume and mass, as well as a significant decrease in CD68+ macrophage count when treated with AZD7507, but not WITT-1 cells[2].
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| Animal Protocol |
Mice: Male CD1 nude mice are given subcutaneous injections of 5 × 105 human ICC cells suspended in a 1:1 mixture of culture media and RGF Matrigel (Gibco) derived from human cell lines WITT-1, CC-LP-1, or SNU-1079 (n = 24 in each case). Two flanks are used to engraft cells, which are then given three weeks to grow into tumors. Using the online program GraphPad, mice are randomized into three groups once palpable tumors have developed. IV injection of liposomal clodronate at 4 μL/g is administered to xenografted mice. Intravenous saline alone or liposomes without clodronate (4 μL/g) are used as the treatment's control. For three weeks, each of these treatments is administered every 48 hours. The CSFR1 inhibitors GW2580 and AZD7507 are prepared in sterile water with 0.1% Tween-80 and 0.5% methylcellulose. The dosage of GW2580 is 160 mg/kg per day, while AZD7507 is administered twice daily at a dose of 100 mg/kg. Water containing 0.1% Tween-80 and 0.5% methylcellulose is given to control animals. Intraperitoneal injections of C-59 (20 mg/kg) or ICG-001 (5 mg/kg) are administered. The physiological saline serves as the vehicle for this. The vehicle is given to control animals alone. Inhibitors and the vehicle are administered three times a week in all cases[2].
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| References |
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| Molecular Formula |
C23H27FN6O3
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|---|---|
| Molecular Weight |
454.497287988663
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| Exact Mass |
454.21
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| Elemental Analysis |
C, 60.78; H, 5.99; F, 4.18; N, 18.49; O, 10.56
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| CAS # |
1041852-85-0
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| Related CAS # |
1041852-85-0
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| PubChem CID |
25001557
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
2.2
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
33
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| Complexity |
652
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
CPDGCAFPSYOTGO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H27FN6O3/c1-14-3-4-17(16(24)11-14)26-21-15-12-19(30-7-5-29(6-8-30)9-10-31)20(33-2)13-18(15)27-28-22(21)23(25)32/h3-4,11-13,31H,5-10H2,1-2H3,(H2,25,32)(H,26,27)
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| Chemical Name |
4-(2-fluoro-4-methylanilino)-6-[4-(2-hydroxyethyl)piperazin-1-yl]-7-methoxycinnoline-3-carboxamide
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| Synonyms |
AZD-7507; AZD7507; AZD 7507
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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 |
| 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) |
DMSO: 91~130 mg/mL (200.2~286.0 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.17 mg/mL (4.77 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 21.7 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: ≥ 2.17 mg/mL (4.77 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 21.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2002 mL | 11.0011 mL | 22.0022 mL | |
| 5 mM | 0.4400 mL | 2.2002 mL | 4.4004 mL | |
| 10 mM | 0.2200 mL | 1.1001 mL | 2.2002 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.
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