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FLT3/D835Y-IN-1

Catalog No. T61977 CAS 2648799-49-7

FLT3/D835Y-IN-1 (compound 13a) is a orally active, and selective inhibitor of FLT3 and FLT3/D835Y, with IC50s of 0.26 nM and 0.18 nM, respectively. FLT3/D835Y-IN-1 has anticancer efficacy, and has research value in AML (acute myeloid leukemia).

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FLT3/D835Y-IN-1, CAS 2648799-49-7

Pack Size	Availability	Price/USD
25 mg	6-8 weeks	$ 1,520.00
50 mg	6-8 weeks	$ 1,980.00
100 mg	6-8 weeks	$ 2,500.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

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Description	FLT3/D835Y-IN-1 (compound 13a) is a orally active, and selective inhibitor of FLT3 and FLT3/D835Y, with IC50s of 0.26 nM and 0.18 nM, respectively. FLT3/D835Y-IN-1 has anticancer efficacy, and has research value in AML (acute myeloid leukemia).
In vitro	FLT3/D835Y-IN-1 (compound 13a), at a concentration of 100 nM over a period of 3 hours, effectively inhibits the proliferation of Ba/F3-FLT3-ITD, Ba/F3-FLT3-ITD/D835Y, Ba/F3-FLT3-ITD-F691L cell lines, and AML cells. When administered at concentrations ranging from 3-30 nM for 16 hours, it markedly suppresses the FLT3, AKT, ERK, and STAT5 signaling pathways. In a cell proliferation assay using these cell lines and AML cells at a 100 nM concentration and a 3-hour incubation, significant inhibition was observed alongside GI50 values of 0.59, 0.73, 5.54, 1.30, 6.20, and 4.58 nM, respectively. Additionally, Western Blot analysis of MOLM14-ITD/D835Y and MOLM14-ITD/F691L cells treated with concentrations of 3, 10, and 30 nM for 16 hours demonstrates a significant reduction in the activity of FLT3, AKT, ERK, and STAT5 pathways 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.

Molecular Weight	403.43
Formula	C22H21N5O3
CAS No.	2648799-49-7

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Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Keywords

FLT3/D835Y-IN-1 2648799-49-7 inhibitor inhibit

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