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H3B-8800

Name: H3B-8800
Brand: TargetMol
SKU: T77595
Price: 297 USD
Availability: InStock
Rating: 5 (10 reviews)

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Synonyms:

Catalog No. T77595 Copy Product Info

Purity: 98.31%

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H3B-8800 is a small-molecule inhibitor and an SF3B1-targeted inhibitor with oral bioactivity and cell permeability. This compound directly binds to the SF3b complex, exhibiting anticancer activity in transfusion-dependent myelodysplastic syndromes and SF3B1-mutant acute myeloid leukemia.

Cas No. 1825302-42-8

Pack Size	Price	USA Stock	Global Stock
1 mg	$297	In Stock	In Stock
5 mg	$786	In Stock	In Stock
50 mg	$2,890	-	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:98.31%

Appearance:Solid

Color:Orange

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COA HNMR HPLC

Product Introduction

Bioactivity

Description	H3B-8800 is a small-molecule inhibitor and an SF3B1-targeted inhibitor with oral bioactivity and cell permeability. This compound directly binds to the SF3b complex, exhibiting anticancer activity in transfusion-dependent myelodysplastic syndromes and SF3B1-mutant acute myeloid leukemia.
Targets & IC50	Panc05.04 cells:13 nM, KPFLC cells (overexpressing human WT):26.5 nM, missense hotspot mutants R175H:8.3 nM, SF3B1:0.3-2 nM, missense hotspot mutants R248H:16.3 nM, missense hotspot mutants R273H:3.2 nM
In vitro	Methods: SF3B1 wild-type and K700E mutant MEC1 chronic lymphocytic leukemia cells and primary CLL cells were incubated with 1–100 nM H3B-8800 for 48 h. Cell viability was detected by flow cytometry, and splicing changes were analyzed by RNA-seq. Results: H3B-8800 killed cells in a dose-dependent manner, showing stronger selectivity for SF3B1 mutant cells, induced widespread splicing alterations, and exhibited synergistic killing effects when combined with venetoclax. [1] Methods: SRSF2-P95H mutant and wild-type bone marrow cells and leukemia cells were treated with gradient concentrations of H3B-8800, and in vitro activity was assessed through cell viability detection and RNA splicing analysis. Results:H3B-8800 selectively killed SRSF2 mutant cells, induced intron retention in GC-rich regions, significantly inhibited aberrant splicing and reduced leukemia cell burden, with weaker effects on wild-type cells. [2]
In vivo	Methods: NSG immunodeficient mice were used to establish a MEC1 cell CLL xenograft model, with SF3B1 wild-type and K700E mutant cells inoculated via tail vein injection. H3B-8800 was administered by daily oral gavage at 6 mg/kg in a solvent mixture containing methylcellulose and ethanol for 10 consecutive days. Results: H3B-8800 significantly reduced bone marrow leukemic infiltration in the SF3B1 K700E group, alleviated hepatosplenomegaly, and delayed tumor infiltration. [3]

Chemical Properties

Molecular Weight	555.71
Formula	C₃₁H₄₅N₃O₆
Cas No.	1825302-42-8
Smiles	O(C(=O)N1CCN(C)CC1)[C@H]2/C=C/[C@H](C)[C@@H](\C(=C\C=C\[C@@H](C)C3=CC=CC=N3)\C)OC(=O)C[C@H](O)CC[C@@]2(C)O
Relative Density.	1.19 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 122.5 mg/mL (220.44 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.7995 mL	8.9975 mL	17.9950 mL	89.9750 mL
5 mM	0.3599 mL	1.7995 mL	3.5990 mL	17.9950 mL
10 mM	0.1799 mL	0.8997 mL	1.7995 mL	8.9975 mL
20 mM	0.0900 mL	0.4499 mL	0.8997 mL	4.4987 mL
50 mM	0.0360 mL	0.1799 mL	0.3599 mL	1.7995 mL
100 mM	0.0180 mL	0.0900 mL	0.1799 mL	0.8997 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.