FLT3/D835Y-IN-1 NEW
| Price | $1520 | $1980 | $2500 |
| Package | 25mg | 50mg | 100mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2025-04-27 |
Product Details
| Product Name: FLT3/D835Y-IN-1 | CAS No.: 2648799-49-7 |
| Supply Ability: 10g | Release date: 2025/04/27 |
Product Introduction
Bioactivity
| Name | FLT3/D835Y-IN-1 |
| Description | FLT3/D835Y-IN-1 (compound 13a) is an orally active, selective inhibitor of FLT3 and FLT3/D835Y with IC50 values of 0.26 nM and 0.18 nM, respectively. It exhibits anticancer efficacy and has research value in AML (acute myeloid leukemia). |
| In vitro | FLT3/D835Y-IN-1 (compound 13a) at 100 nM for 3 hours effectively inhibits the proliferation of Ba/F3-FLT3-ITD, Ba/F3-FLT3-ITD/D835Y, Ba/F3-FLT3-ITD-F691L, and AML cells. At 3-30 nM for 16 hours, it markedly suppresses FLT3, AKT, ERK, and STAT5 signaling. A 100 nM 3-hour incubation resulted in significant inhibition with GI50 values of 0.59, 0.73, 5.54, 1.30, 6.20, and 4.58 nM. Western Blot analysis of MOLM14-ITD/D835Y and MOLM14-ITD/F691L cells treated with 3, 10, and 30 nM for 16 hours showed a significant reduction in FLT3, AKT, ERK, and STAT5 pathway activities at lower doses. |
| In vivo | Administering FLT3/D835Y-IN-1 at a dosage of 10 mg/kg interperitoneally (IP) daily for six days per week notably inhibits tumor proliferation and demonstrates strong antitumor efficacy against MOLM14-ITD/D835Y cells. Conversely, administering a single dose of 10 mg/kg intravenously (IV) or orally reveals a considerably low area under the curve (AUC) and elevated clearance rates in pharmacokinetic studies, indicating rapid drug elimination. Additionally, pharmacokinetic parameters assessed in ICR mice include an AUC of 1360 ± 110 ng*h/mL, clearance rate (CL) of 6.96 ± 0.66 L/h/kg, steady-state volume of distribution (Vss) of 14.8 ± 0.7 L/kg, and a half-life (T1/2) of 1.5 ± 0.1 hours. In trials involving NOD/SCID mice (9 per group, 6 weeks old, male), the compound significantly reduced tumor size when given IP daily at 10 mg/kg from day 7 to 29. Similarly, in ICR mice (7–8 weeks old, male), a single dose of the compound, dissolved in 10% DMSO, 40% PEG400, and 50% PBS, administered IV or orally showed significantly low AUC and high clearance. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Company Profile Introduction
TargetMol Chemicals Inc. is headquartered in Boston, MA, and specializes in products and services that serve the research needs of chemical and biological scientists worldwide. With a client base in 40+ countries, TargetMol has evolved into one of the biggest global research suppliers for compound libraries and small molecule compounds.
170+ Compound Libraries， 10000+ Noval Small Molecucles，16000+ Nature Compounds
TargetMol diligently updates and offers over 170 types of compound libraries and a wide range of high-quality research chemicals, including inhibitors, activators, natural products, peptides, antibodies , and novel life-science kits for laboratory and scientific use. In addition, our lab allows us to conduct CADD (computer-aided drug design) and chemical synthesis to meet the customization needs of our clients.
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United States- Since: 2011-01-07
- Address: 36 Washington Street, Wellesley Hill, Massachusetts, USA
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