SX-682 |
カタログ番号GC38204
One-Click Copy Product Info
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SX-682はCXCR1とCXCR2の経口生物利用可能な小分子阻害剤であり、IC50値はそれぞれ31と21nMである。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1648843-04-2
Sample solution is provided at 25 µL, 10mM.
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SX-682はCXCR1とCXCR2の経口生物利用可能な小分子阻害剤であり、IC50値はそれぞれ31と21nMである[1]。SX-682は、間葉系から上皮性腫瘍表現型への転換を効果的に促進し、同時に免疫媒介の細胞毒性への腫瘍細胞の感受性を増強する[2]。SX-682は抗癌剤として広く使われ、大腸癌の進行を阻害してきている[3]。
体外で、SX-682（5μM）で4日間処理した結果、B16F0とB16F10細胞の成長を著しく阻害し、Cxcl1と血管内皮増殖因子（VEGF）の産生を減らした[4]。2.5µMのSX-682と25µg/mLのbintrafusp alfaの3日間の併用処理は、4T1細胞の著しい凝集を起こし、E-カドヘリンの発見を上方制御し、間葉系細胞ビメンチン、間葉系転写因子SnailとZeb-1の発見を下げた[5]。10µMのSX-682で72時間事前処理した結果、docetaxelに対するUM-SCC-11B細胞の感受性を著しく増強し、細胞の生存率を大きく減らした[6]。
体内で、200mg/kgのSX-682を2週間、毎日二回経口投与した結果、マウスで、腫瘍関連の好中球の含有量を減らさずに、肺腫瘍の成長を著しく阻害した[7]。SX-682（0.756g/kg/日；経口投与）と抗PD-1抗体の3週間の併用処理は、Rich1.1黒色腫細胞異種移植マウスモデルで、腫瘍の成長を著しく阻害し、腫瘍内で骨髄系由来の抑制細胞（MDSC）を減らし、腫瘍内でCXCL11を発見するB1b細胞を増やした[8]。
References:
[1] Maeda D Y, Peck A M, Schuler A D, et al. Boronic acid-containing CXCR1/2 antagonists: Optimization of metabolic stability, in vivo evaluation, and a proposed receptor binding model[J]. Bioorganic & medicinal chemistry letters, 2015, 25(11): 2280-2284.
[2] Horn L, Hamilton D, Maeda D, et al. Abstract B04: Multimodal cancer immunotherapy combining IL-8 inhibition, adenovirus vaccine, IL-15 super agonist, and anti-PD-L1/TGFβRII agent reduces mesenchymalization and enhances anti-tumor efficacy[J]. Cancer Immunology Research, 2020, 8(4_Supplement): B04-B04.
[3] Sherry C, Dadgar N, Liu Z, et al. The Interleukin-8-CXCR1/2 Axis as a Therapeutic Target in Peritoneal Carcinomatosis[J]. Current Oncology, 2025, 32(9): 496.
[4] Yang J, Bergdorf K, Yan C, et al. CXCR2 expression during melanoma tumorigenesis controls transcriptional programs that facilitate tumor growth[J]. Molecular Cancer, 2023, 22(1): 92.
[5] Horn L A, Riskin J, Hempel H A, et al. Simultaneous inhibition of CXCR1/2, TGF-β, and PD-L1 remodels the tumor and its microenvironment to drive antitumor immunity[J]. Journal for immunotherapy of cancer, 2020, 8(1): e000326.
[6] Horn L A, Lind H, Fousek K, et al. Inhibition of the chemokine receptors CXCR1 and CXCR2 synergizes with docetaxel for effective tumor control and remodeling of the immune microenvironment of HPV-negative head and neck cancer models[J]. Journal of Experimental & Clinical Cancer Research, 2024, 43(1): 318
[7] Kwak J W, Nguyen H Q, Camai A, et al. CXCR1/2 antagonism inhibits neutrophil function and not recruitment in cancer[J]. Oncoimmunology, 2024, 13(1): 2384674.
[8] Yang J, Yan C, Vilgelm A E, et al. Targeted deletion of CXCR2 in myeloid cells alters the tumor immune environment to improve antitumor immunity[J]. Cancer immunology research, 2021, 9(2): 200-213.
| 細胞実験[1]: | |
細胞株 | 4T1細胞 |
準備方法 | 4T1細胞をそれぞれ、10% FBSを含有するIMDM培地で2.5µM SX-682、25µg/ml bintrafusp alfa、または2.5µM SX-682と25µg/ml bintrafusp alfaの併用で72時間培養した。細胞におけるE-カドヘリンと間葉系転写因子の発見を分析した。 |
反応条件 | 2.5µM；72時間 |
アプリケーション | SX-682の処理は、4T1細胞で、E-カドヘリンの発見を上方制御し、間葉系転写因子SnailとZeb-1の発見を下げた。 |
| 動物実験 [2]: | |
動物モデル | C57BL/6マウス |
準備方法 | 相同なRich1.1黒色腫細胞BrafV637E PtenR74X, Q396Xを、免疫能力を持つC57BL/6マウスに皮下移植した。SX-682（0.756g/kg）を含有する飼料をC57BL/6マウスに投与し、同時に抗PD-1抗体（100μg/マウス）、または対照物IgGを腹腔内注射し、或いはSX-682なしで溶媒対照飼料を投与し、抗PD-1抗体または同種類の対照IgGを隔日で腹腔内注射した。3週間の処理後、マウスの肺組織を分析のために除去した。 |
投与形態 | 0.756g/kg/日、3週間；経口投与 |
アプリケーション | SX-682と抗PD-1抗体の併用処理は、マウスで肺腫瘍の成長を著しく阻害し、腫瘍内で骨髄系由来の抑制細胞（MDSC）を減らし、腫瘍内でCXCL11を発見するB1b細胞を増やした。 |
References: | |
| Cas No. | 1648843-04-2 | SDF | |
| Canonical SMILES | O=C(NC1=CC=C(F)C=C1)C(C=N2)=CN=C2SCC3=CC(OC(F)(F)F)=CC=C3B(O)O | ||
| Formula | C19H14BF4N3O4S | M.Wt | 467.2 |
| 溶解度 | DMSO: 250 mg/mL (535.10 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.1404 mL | 10.7021 mL | 21.4041 mL |
| 5 mM | 428.1 μL | 2.1404 mL | 4.2808 mL |
| 10 mM | 214 μL | 1.0702 mL | 2.1404 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)