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References |
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PMID: 36933582. 4: An X, Wang J, Tong L, Zhang X, Fu H, Zhang J, Xie H, Huang Y, Jia H. 18F-Labeled o‑aminopyridyl alkynyl radioligands targeting colony- stimulating factor 1 receptor for neuroinflammation imaging. Bioorg Med Chem. 2023 Apr 1;83:117233. doi: 10.1016/j.bmc.2023.117233. Epub 2023 Mar 8. PMID: 36933438. 5: Thongchot S, Duangkaew S, Yotchai W, Maungsomboon S, Phimolsarnti R, Asavamongkolkul A, Thuwajit P, Thuwajit C, Chandhanayingyong C. Novel CSF1R-positive tenosynovial giant cell tumor cell lines and their pexidartinib (PLX3397) and sotuletinib (BLZ945)-induced apoptosis. Hum Cell. 2023 Jan;36(1):456-467. doi: 10.1007/s13577-022-00823-0. Epub 2022 Dec 2. PMID: 36456782; PMCID: PMC9813176. 6: Kesarwani P, Kant S, Zhao Y, Miller CR, Chinnaiyan P. The Influence of the Ketogenic Diet on the Immune Tolerant Microenvironment in Glioblastoma. Cancers (Basel). 2022 Nov 11;14(22):5550. doi: 10.3390/cancers14225550. PMID: 36428642; PMCID: PMC9688691. 7: Pognan F, Buono C, Couttet P, Galarneau JR, Timsit Y, Wolf A. Liver enzyme delayed clearance in rat treated by CSF1 receptor specific antagonist Sotuletinib. Curr Res Toxicol. 2022 Oct 29;3:100091. doi: 10.1016/j.crtox.2022.100091. PMID: 36353522; PMCID: PMC9637862. 8: Chokr SM, Milinkeviciute G, Jimenez GA, Abubakr H, Cramer KS. Long-term microglia depletion impairs synapse elimination and auditory brainstem function. Sci Rep. 2022 Nov 2;12(1):18521. doi: 10.1038/s41598-022-23250-5. PMID: 36323869; PMCID: PMC9630367. 9: Xie X, Feng Y, Zhang H, Su Q, Song T, Yang G, Li N, Wei X, Li T, Qin X, Li S, Wu C, Zhang X, Wang G, Liu Y, Yang H. Remodeling tumor immunosuppressive microenvironment via a novel bioactive nanovaccines potentiates the efficacy of cancer immunotherapy. Bioact Mater. 2022 Mar 11;16:107-119. doi: 10.1016/j.bioactmat.2022.03.008. Erratum in: Bioact Mater. 2022 Sep 07;21:239-240. PMID: 35386322; PMCID: PMC8958467. 10: Hwang D, Seyedsadr MS, Ishikawa LLW, Boehm A, Sahin Z, Casella G, Jang S, Gonzalez MV, Garifallou JP, Hakonarson H, Zhang W, Xiao D, Rostami A, Zhang GX, Ciric B. CSF-1 maintains pathogenic but not homeostatic myeloid cells in the central nervous system during autoimmune neuroinflammation. Proc Natl Acad Sci U S A. 2022 Apr 5;119(14):e2111804119. doi: 10.1073/pnas.2111804119. Epub 2022 Mar 30. PMID: 35353625; PMCID: PMC9168454. 11: Kosti CN, Vaitsi PC, Pappas AG, Iliopoulou MP, Psarra KK, Magkouta SF, Kalomenidis IT. CSF1/CSF1R signaling mediates malignant pleural effusion formation. JCI Insight. 2022 Mar 22;7(6):e155300. doi: 10.1172/jci.insight.155300. PMID: 35315360; PMCID: PMC8986064. 12: Klemm F, Möckl A, Salamero-Boix A, Alekseeva T, Schäffer A, Schulz M, Niesel K, Maas RR, Groth M, Elie BT, Bowman RL, Hegi ME, Daniel RT, Zeiner PS, Zinke J, Harter PN, Plate KH, Joyce JA, Sevenich L. Compensatory CSF2-driven macrophage activation promotes adaptive resistance to CSF1R inhibition in breast-to-brain metastasis. Nat Cancer. 2021 Oct;2(10):1086-1101. doi: 10.1038/s43018-021-00254-0. Epub 2021 Oct 18. PMID: 35121879. 13: Borse V, Kaur T, Hinton A, Ohlemiller K, Warchol ME. Programmed Cell Death Recruits Macrophages Into the Developing Mouse Cochlea. Front Cell Dev Biol. 2021 Dec 9;9:777836. doi: 10.3389/fcell.2021.777836. PMID: 34957108; PMCID: PMC8696258. 14: Wies Mancini VSB, Di Pietro AA, de Olmos S, Silva Pinto P, Vence M, Marder M, Igaz LM, Marcora MS, Pasquini JM, Correale JD, Pasquini LA. Colony- stimulating factor-1 receptor inhibition attenuates microgliosis and myelin loss but exacerbates neurodegeneration in the chronic cuprizone model. J Neurochem. 2022 Mar;160(6):643-661. doi: 10.1111/jnc.15566. Epub 2022 Jan 9. PMID: 34935149. 15: Sun X, Zhang J, Zhao X, Yang C, Shi M, Zhang B, Hu H, Qiao M, Chen D, Zhao X. Binary regulation of the tumor microenvironment by a pH-responsive reversible shielding nanoplatform for improved tumor chemo-immunotherapy. Acta Biomater. 2022 Jan 15;138:505-517. doi: 10.1016/j.actbio.2021.11.017. Epub 2021 Nov 16. PMID: 34798317. 16: Pfirschke C, Zilionis R, Engblom C, Messemaker M, Zou AE, Rickelt S, Gort- Freitas NA, Lin Y, Bill R, Siwicki M, Gungabeesoon J, Sprachman MM, Marquard AN, Rodell CB, Cuccarese MF, Quintana J, Ahmed MS, Kohler RH, Savova V, Weissleder R, Klein AM, Pittet MJ. Macrophage-Targeted Therapy Unlocks Antitumoral Cross- talk between IFNγ-Secreting Lymphocytes and IL12-Producing Dendritic Cells. Cancer Immunol Res. 2022 Jan;10(1):40-55. doi: 10.1158/2326-6066.CIR-21-0326. Epub 2021 Dec 1. PMID: 34795032; PMCID: PMC10132467. 17: van der Wildt B, Miao Z, Reyes ST, Park JH, Klockow JL, Zhao N, Romero A, Guo SG, Shen B, Windhorst AD, Chin FT. BLZ945 derivatives for PET imaging of colony stimulating factor-1 receptors in the brain. Nucl Med Biol. 2021 Sep- Oct;100-101:44-51. doi: 10.1016/j.nucmedbio.2021.06.005. Epub 2021 Jun 23. PMID: 34174546. 18: Fang Y, He Y, Wu C, Zhang M, Gu Z, Zhang J, Liu E, Xu Q, Asrorov AM, Huang Y. Magnetism-mediated targeting hyperthermia-immunotherapy in "cold" tumor with CSF1R inhibitor. Theranostics. 2021 May 3;11(14):6860-6872. doi: 10.7150/thno.57511. PMID: 34093858; PMCID: PMC8171105. 19: Magkouta SF, Vaitsi PC, Pappas AG, Iliopoulou M, Kosti CN, Psarra K, Kalomenidis IT. CSF1/CSF1R Axis Blockade Limits Mesothelioma and Enhances Efficiency of Anti-PDL1 Immunotherapy. Cancers (Basel). 2021 May 22;13(11):2546. doi: 10.3390/cancers13112546. PMID: 34067348; PMCID: PMC8196870. 20: Liaw K, Reddy R, Sharma A, Li J, Chang M, Sharma R, Salazar S, Kannan S, Kannan RM. Targeted systemic dendrimer delivery of CSF-1R inhibitor to tumor- associated macrophages improves outcomes in orthotopic glioblastoma. Bioeng Transl Med. 2020 Dec 11;6(2):e10205. doi: 10.1002/btm2.10205. PMID: 34027092; PMCID: PMC8126814.
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Molecular Formula |
C20H24CL2N4O3S
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Molecular Weight |
471.397
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Exact Mass |
0
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Elemental Analysis |
C, 50.96; H, 5.13; Cl, 15.04; N, 11.89; O, 10.18; S, 6.80
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CAS # |
2222138-40-9
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Related CAS # |
Sotuletinib;953769-46-5;Sotuletinib hydrochloride;2222138-31-8
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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.[H]Cl
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InChi Key |
ZIHWHYXECXSBNA-LVVRIOTCSA-N
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InChi Code |
InChI=1S/C20H22N4O3S.2ClH/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);2*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 dihydrochloride
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Synonyms |
Sotuletinib dihydrochloride; BLZ945; BLZ 945; BLZ-945.Sotuletinib;
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.1213 mL | 10.6067 mL | 21.2134 mL | |
5 mM | 0.4243 mL | 2.1213 mL | 4.2427 mL | |
10 mM | 0.2121 mL | 1.0607 mL | 2.1213 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.