AS-99 free base
Based on 2 publication(s) in Google Scholar
AS-99 is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.57%
- CAS 番号: 2323623-93-2
- 分子式: C27H30F3N5O3S2
- 分子量:593.68
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 AS-99 free base
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Customer Validation & Images
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In Vivo Efficacy Study
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IHC
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In Vivo Imaging
Histone Methyltransferase アイソフォーム固有の製品をすべて表示
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生物活性
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ASH1L/KMT2H |
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Cell Line
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Type | Value | Description | References |
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| KOPN-8 | GI50 |
1.8 μM
Compound: 46; AS-99
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Growth inhibition of human KOPN-8 cells
Growth inhibition of human KOPN-8 cells
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[PMID: 38805937] |
| MOLM-13 | GI50 |
1.8 μM
Compound: 46; AS-99
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Growth inhibition of human MOLM-13 cells
Growth inhibition of human MOLM-13 cells
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[PMID: 38805937] |
| MV4-11 | GI50 |
1.8 μM
Compound: 46; AS-99
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Growth inhibition of human MV4-11 cells after 7 days by WST-8 assay
Growth inhibition of human MV4-11 cells after 7 days by WST-8 assay
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[PMID: 38805937] |
AS-99 is tested against a panel of 20 histone methyltransferases, including NSD1, NSD2, NSD3, and SETD2. NO significant inhibition is observed at 50 µM of AS-99 on any of the tested histone methyltransferases, indicating over 100-fold selectivity towards ASH1L[1].
AS-99 shows a several fold weaker effect on the proliferation of leukemia cells without MLL1 translocations, such as SET2 and K562, with no or limited effects at 10 µM or higher concentrations[1].
AS-99 (1-8 µM; 7 days) also induces apoptosis in the MLL leukemia cells, but not in the K562 cells, as assessed by the quantification of the Annexin V positive cells[1].
AS-99 suppresses MLL fusion driven transcriptional programs[1].
AS-99 results in a reduced number of H3K36me2 peaks when compared to the DMSO-treated cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MOLM13 cells
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Concentration:2-6 µM
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Incubation Time:7 days
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Result:Led to a dose-dependent downregulation of canonical MLL fusion target genes required for leukemogenesis including MEF2C, DLX2, FLT3, and HOXA9.
AS-99 is used for in vivo studies in mice, which reveals favorable exposure in plasma upon i.v. and i.p. administration (AUC = 9701 hr* ng/mL and 10,699 hr* ng/mL, respectively), suitable half-life (~5–6 h) and Cmax >10 µM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:8- to 10-week old female NSG mice (bearing MV4;11 cells)[1]
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Dosage:30 mg/kg
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Administration:I.p.; q.d., treated for 14 consecutive days
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Result:Reduced the leukemia burden in the xenotransplantation mouse model of MLL leukemia without affecting blood counts in normal mice.
化学情報
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CAS 番号 2323623-93-2
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性状 Solid
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分子量 593.68
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分子式 C27H30F3N5O3S2
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Color White to off-white
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SMILES
O=C(C1CN(C)C1)NCC2=CC3=C(C=C2)C(C4=CC=CC(C(N)=S)=C4)=CN3C5CCN(S(=O)(C(F)(F)F)=O)CC5
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Nat Commun
Histone methyltransferase ASH1L primes metastases and metabolic reprogramming of macrophages in the bone niche. [Abstract]2025 May 20;16(1):4681. PMID: 40394007
AS-99 free base purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 May 20;16(1):4681. [Abstract]
AS-99 (25 mg/kg, i.p.) treatment significantly suppressed metastases to bone and prolonged the overall survival of mice.
AS-99 free base purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 May 20;16(1):4681. [Abstract]
Multiplex IHC staining of TAMs in bone tumors treated with AS-99 (i.p., 25 mg/kg).
AS-99 free base purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 May 20;16(1):4681. [Abstract]
2 × 106 PC-3M cells were intracardiac injected into male nude mice, followed by treatment of vehicle or ASH1L inhibitor AS-99 (i.p., 25 mg/kg). Bioluminescent imaging and intensity quantification of metastatic tumors on Day 34 are presented.
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Adv Sci (Weinh)
ASH1L in Hepatoma Cells and Hepatic Stellate Cells Promotes Fibrosis-Associated Hepatocellular Carcinoma by Modulating Tumor-Associated Macrophages. [Abstract]2024 Dec;11(45):e2404756. PMID: 39377228
溶剤 & 溶解度
DMSO : ≥ 100 mg/mL (168.44 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (278 KB)
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SDS (252 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6844 mL | 8.4220 mL | 16.8441 mL | 42.1102 mL |
| 5 mM | 0.3369 mL | 1.6844 mL | 3.3688 mL | 8.4220 mL | |
| 10 mM | 0.1684 mL | 0.8422 mL | 1.6844 mL | 4.2110 mL | |
| 15 mM | 0.1123 mL | 0.5615 mL | 1.1229 mL | 2.8073 mL | |
| 20 mM | 0.0842 mL | 0.4211 mL | 0.8422 mL | 2.1055 mL | |
| 25 mM | 0.0674 mL | 0.3369 mL | 0.6738 mL | 1.6844 mL | |
| 30 mM | 0.0561 mL | 0.2807 mL | 0.5615 mL | 1.4037 mL | |
| 40 mM | 0.0421 mL | 0.2106 mL | 0.4211 mL | 1.0528 mL | |
| 50 mM | 0.0337 mL | 0.1684 mL | 0.3369 mL | 0.8422 mL | |
| 60 mM | 0.0281 mL | 0.1404 mL | 0.2807 mL | 0.7018 mL | |
| 80 mM | 0.0211 mL | 0.1053 mL | 0.2106 mL | 0.5264 mL | |
| 100 mM | 0.0168 mL | 0.0842 mL | 0.1684 mL | 0.4211 mL |
AS-99 free base 関連分類
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