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| ln Vitro |
In bone marrow-derived macrophages (BMDM), sotuletinib hydrochloride suppresses CSF-1 suspension proliferation (EC50=67 nM) and decreases CSF-1R phosphorylation, which is likewise inhibited by CSF-1R inhibitors. Crucially, sotuletinib hydrochloride in culture did not affect ischemia in any PDG-derived tumor cell lines (all Csf-1r negative), U-87 MG human neuroastroma cells, or the formation of PDG spheroids by tumor cells. It also decreased the viability of CRL-2467 astrocytes, Ink4a/Arf/BMDM (PDG genetic background), and NOD/SCID BMDM. ..As a result, solutetinib hydrochloride directly affects neuroastroma cell ischemia and prevents CSF-1R-disrupted macrophage ischemia [1].
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| ln Vivo |
In the cohort treated with vehicles, the median survival was 5.7 weeks. Long-term survival was markedly increased by sotuletinib hydrochloride; 64.3% of patients receiving vehicle treatment reached the 26-week trial endpoint. This endpoint was selected because Ink4a/Arf/EGFR starts to spontaneously generate tumors at about 30 weeks, including sarcomas and severe tumors. In line with histological investigations, solutetinib hydrochloride was well tolerated over the long run with no discernible side effects. Tumors from all mice treated with vehicles had high-grade neuroastromas, according to histological grading. On the other hand, solutetinib hydrochloride-treated animals showed noticeably smaller tumors overall, and 55.6% of asymptomatic mice had no visible lesions at the end of the experiment [1]. Sotutinib hydrochloride-treated tumors and the stroma around them displayed decreased CSF1R staining, and CSF1R+ stromal macrophages were considerably lower than those of vehicle-treated tumors (P<0.05) [2].
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| References |
[1]. Pyonteck SM, et al. CSF-1R inhibition alters macrophage polarization and blocks glioma progression. Nat Med. 2013 Oct;19(10):1264-72.
[2]. Strachan DC, et al. CSF1R inhibition delays cervical and mammary tumor growth in murine models by attenuating the turnover of tumor-associated macrophages and enhancing infiltration by CD8+ T cells. Oncoimmunology. 2013 Dec 1;2(12):e26968. |
| Molecular Formula |
C20H23CLN4O3S
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|---|---|
| Molecular Weight |
434.939
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| Exact Mass |
0
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| Elemental Analysis |
C, 55.23; H, 5.33; Cl, 8.15; N, 12.88; O, 11.04; S, 7.37
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| CAS # |
2222138-31-8
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| Related CAS # |
Sotuletinib;953769-46-5;Sotuletinib dihydrochloride;2222138-40-9
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| SMILES |
O=C(NC)C1=NC=CC(OC2=CC=C3N=C(N[C@H]4[C@H](O)CCCC4)SC3=C2)=C1.[H]Cl
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| InChi Key |
IHWOVMRZEIHNGY-SATBOSKTSA-N
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| InChi Code |
InChI=1S/C20H22N4O3S.ClH/c1-21-19(26)16-10-13(8-9-22-16)27-12-6-7-15-18(11-12)28-20(24-15)23-14-4-2-3-5-17(14)25;/h6-11,14,17,25H,2-5H2,1H3,(H,21,26)(H,23,24);1H/t14-,17-;/m1./s1
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| Chemical Name |
4-((2-(((1R,2R)-2-hydroxycyclohexyl)amino)benzo[d]thiazol-6-yl)oxy)-N-methylpicolinamide hydrochloride
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| Synonyms |
Sotuletinib HCl; Sotuletinib hydrochloride, Sotuletinib monohydrochloride, BLZ945; BLZ 945; BLZ-945;
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| Solubility (In Vitro) |
H2O : ~100 mg/mL (~229.92 mM)
DMSO : ~100 mg/mL (~229.92 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.75 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 25.0 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: ≥ 2.5 mg/mL (5.75 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 25.0 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: ≥ 2.5 mg/mL (5.75 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 | 2.2992 mL | 11.4958 mL | 22.9917 mL | |
| 5 mM | 0.4598 mL | 2.2992 mL | 4.5983 mL | |
| 10 mM | 0.2299 mL | 1.1496 mL | 2.2992 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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