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| Cas No.: | 1041852-85-0 |
| Chemical Name: | AZD7507 |
| Synonyms: | AZD7507;4-(2-fluoro-4-methylanilino)-6-[4-(2-hydroxyethyl)piperazin-1-yl]-7-methoxycinnoline-3-carboxamide;AMY16926;BDBM50492685;A16886;D77979;4-((2-fluoro-4-methylphenyl)amino)-6-(4-(2-hydroxyethyl)piperazin-1-yl)-7-methoxycinnoline-3-carboxamide |
| SMILES: | FC1C=C(C)C=CC=1NC1=C(C(N)=O)N=NC2C=C(C(=CC=21)N1CCN(CCO)CC1)OC |
| Formula: | C23H27FN6O3 |
| M.Wt: | 454.506 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | AZD7507 is a potent and orally active CSF-1R inhibitor, with antitumor activity. |
| Target: | CSF-1R[1] |
| In Vivo: | AZD7507 has good rat oral PK, with in vivo clearance of 7 mL/min/kg and 42% bioavailability. In the canine L-type Ca channel assay, the IC50 is >20 μM[1]. AZD7507 significantly decreases the number of CD68+ macrophages in mice, and also reduces the volume and mass in mice bearing CC-LP-1 and SNU-1079 cells, but not WITT-1 cells[2]. |
| In Vitro: | AZD7507 (Compound 31) inhibits the proliferation of 3T3 cells engineered to express CSF-1R and stimulated with CSF-1 (IC50, 32 nM), shows inhibitory activity against hERG and NaV1.5, with IC50s of >30 and 26 μM[1]. |
| Animal Administration: | Mice[2] Male CD1 nude mice are injected subcutaneously with 5 × 105 human ICC cells from human cell line WITT-1, CC-LP-1, or SNU-1079 (n = 24 in all cases) suspended in culture media/RGF Matrigel (Gibco) mix (1:1). Cells are engrafted bilaterally in the flank and allowed to form tumors over 3 weeks. Once palpable tumors have formed, mice are randomized into 3 groups using GraphPad online software. Xenografted mice are injected with liposomal clodronate at 4 μL/g intravenously. The control for this treatment is saline alone or liposomes not containing clodronate (both given at 4 μL/g intravenously). All of these treatments are given every 48 hours for 3 weeks. CSFR1 inhibitors AZD7507 and GW2580 are made up in sterile water containing 0.5% methylcellulose and 0.1% Tween-80. AZD7507 is given twice daily at 100 mg/kg, whereas GW2580 is given daily at 160 mg/kg. Control animals are given water containing 0.5% methylcellulose and 0.1% Tween-80. ICG-001 (5 mg/kg) or C-59 (20 mg/kg) is given by intraperitoneal injection. The vehicle for this is physiological saline. Control animals are given vehicle alone. In all cases inhibitors and vehicle are given 3 times per week[2]. |
| References: | [1]. Scott DA, et al. Mitigation of cardiovascular toxicity in a series of CSF-1R inhibitors, and the identification of AZD7507. Bioorg Med Chem Lett. 2013 Aug 15;23(16):4591-6. [2]. Boulter L, et al. WNT signaling drives cholangiocarcinoma growth and can be pharmacologically inhibited. Send to J Clin Invest. 2015 Mar 2;125(3):1269-85. |
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| 2018-0101 |
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| 2018-0101 |
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| 2018-0101 |
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