Sotuletinib (BLZ945)

製品コードS7725 バッチS772506

印刷

化学情報

Chemical Structure Synonyms Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C20H22N4O3S
分子量 398.48 CAS No. 953769-46-5
Solubility (25°C)* 体外 DMSO 80 mg/mL (200.76 mM)
Ethanol (warmed with 50ºC water bath) 2 mg/mL (5.01 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Sotuletinib (BLZ945) is an orally active, potent and selective CSF-1R inhibitor with IC50 of 1 nM, >1000-fold selective against its closest receptor tyrosine kinase homologs.
in vitro

In bone marrow-derived macrophages (BMDMs), Sotuletinib (BLZ945) specifically inhibits CSF-1-dependent proliferation with EC50 of 67nM, and decreases CSF-1R phosphorylation. It blocks the reciprocal effects between macrophages and glioma cells on the survival, proliferation and/ or polarization of each other to promote tumorigenesis. [1]
in vivo

Sotuletinib (BLZ945) blocks tumor progression and significantly improves survival via CSF-1R inhibition in glioma-bearing mice. It also inhibits orthotopic tumor growth of patient-derived proneural tumor spheres and cell lines in vivo. [1] This compound (200 mg/kg, p.o.) decreases the growth of malignant cells in both mouse mammary tumor virus-driven polyomavirus middle T antigen (MMTV-PyMT) model of mammary carcinogenesis and keratin 14-expressing human papillomavirus type 16 (K14-HPV-16) transgenic model of cervical carcinogenesis. [2]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Glioma cell lines, BMDM, CRL-2467, HUVEC and HBMEC cell lines
濃度 ~6700 nM
反応時間 96 hours
実験の流れ

Cell growth rate is determined using the MTT cell proliferation kit. Briefly, cells are plated in triplicate in 96-well plates: 1,000 cells per well for glioma cell lines, 5 x 1,000 cells per well for BMDM and CRL-2467, and 2.5 x 1,000 cells per well for HUVEC and HBMEC cell lines. For all experiments, media is changed every 48 h. Cells are grown in the presence or absence of 6.7–6,700 nM of Sotuletinib (BLZ945), or 8 μg/mL of CSF-1R neutralizing antibody. BMDM and CRL-2467 cells were supplemented with 10 ng/mL and 30 ng/ mL recombinant mouse CSF-1, respectively. Reduction of the MTT substrate is detected by colorimetric analysis using a plate reader as per the manufacturer’s protocol, and measured at 595 nm and 750 nm on a spectraMax 340pc plate reader.
動物実験 動物モデル Female MMTV-PyMT transgenic mice
投薬量 200 mg/kg
投与方法 p.o.

参考

  • https://pubmed.ncbi.nlm.nih.gov/24056773/
  • https://pubmed.ncbi.nlm.nih.gov/24498562/

カスタマーフィードバック

, , Clin Cancer Res, 2017, 23(20):6021-6030

Data from [Data independently produced by , , Cancer Res, 2018, 78(15):4253-4269]

Data from [Data independently produced by , , Clin Cancer Res, 2016, 22(15):3849-59.]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

CSF1R+ myeloid-monocytic cells drive CAR-T cell resistance in aggressive B cell lymphoma [ Cancer Cell, 2025, S1535-6108(25)00222-3] PubMed: 40513575
MORF4L2 induces immunosuppressive microenvironment and immunotherapy resistance through GRHL2/MORF4L2/H4K12Ac/CSF1 axis in triple-negative breast cancer [ Biomark Res, 2025, 13(1):6] PubMed: 39780291
Macrophages excite muscle spindles with glutamate to bolster locomotion [ Nature, 2024, 10.1038/s41586-024-08272-5] PubMed: 39633045
Lactate dehydrogenase A regulates tumor-macrophage symbiosis to promote glioblastoma progression [ Nat Commun, 2024, 15(1):1987] PubMed: 38443336
Assessing Novel Antibody-Based Therapies in Reconstructive 3D Cell Models of the Tumor Microenvironment [ Adv Biol (Weinh), 2024, 8(12):e2400431] PubMed: 39601467
Human microglia maturation is underpinned by specific gene regulatory networks [ Immunity, 2023, 56(9):2152-2171.e13] PubMed: 37582369
Engineering an inhibitor-resistant human CSF1R variant for microglia replacement [ J Exp Med, 2023, 220(3)e20220857] PubMed: 36584406
Hypoxia-driven protease legumain promotes immunosuppression in glioblastoma [ Cell Rep Med, 2023, S2666-3791(23)00415-9] PubMed: 37858339
LDHA-regulated tumor-macrophage symbiosis promotes glioblastoma progression [ Res Sq, 2023, 10.1146/annurev-genet-022123-113904] PubMed: 37886538
Patient-Specific Vascularized Tumor Model: Blocking TAM Recruitment with Multispecific Antibodies Targeting CCR2 and CSF-1R [ bioRxiv, 2023, 2023.11.28.568627] PubMed: 38076998

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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