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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.57%
- No. CAS: 2323623-93-2
- Fòrmula: C27H30F3N5O3S2
- Peso molecular:593.68
-
Almacenamiento: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]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) AS-99 free base
More
Customer Validation & Images
-
In Vivo Efficacy Study
-
IHC
-
In Vivo Imaging
Ver todos los productos específicos de isoformas Histone Methyltransferase
More
Actividad biológica
|
ASH1L/KMT2H |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| KOPN-8 | GI50 |
1.8 μM
Compound: 46; AS-99
|
Growth inhibition of human KOPN-8 cells
Growth inhibition of human KOPN-8 cells
|
[PMID: 38805937] |
| MOLM-13 | GI50 |
1.8 μM
Compound: 46; AS-99
|
Growth inhibition of human MOLM-13 cells
Growth inhibition of human MOLM-13 cells
|
[PMID: 38805937] |
| MV4-11 | GI50 |
1.8 μM
Compound: 46; AS-99
|
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
|
[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.
-
Cell Line:MOLM13 cells
-
Concentration:2-6 µM
-
Incubation Time:7 days
-
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.
-
Animal Model:8- to 10-week old female NSG mice (bearing MV4;11 cells)[1]
-
Dosage:30 mg/kg
-
Administration:I.p.; q.d., treated for 14 consecutive days
-
Result:Reduced the leukemia burden in the xenotransplantation mouse model of MLL leukemia without affecting blood counts in normal mice.
Chemical Information
-
No. CAS 2323623-93-2
-
Appearance Solid
-
Peso molecular 593.68
-
Fòrmula C27H30F3N5O3S2
-
Color White to off-white
-
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
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
-
Journal Impact Factor
-
Most Recent
-
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.
-
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
Solvente y solubilidad
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
-
Ficha de datos (278 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
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 Related Classifications
HY-141429 Related Classifications
Powered by Bioz