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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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Catalog No. T77595Cas No. 1825302-42-8

H3B-8800 is an SF3B1 modulator that can be used to study transfusion-dependent anemia.

H3B-8800

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Purity: 98.31%

Catalog No. T77595Cas No. 1825302-42-8

H3B-8800 is an SF3B1 modulator that can be used to study transfusion-dependent anemia.

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

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:98.31%

Appearance:Solid

Color:Orange

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COA HPLC HNMR

Product Introduction

Bioactivity

Description	H3B-8800 is an SF3B1 modulator that can be used to study transfusion-dependent anemia.
Targets&IC50	SF3B1:0.3-2 nM, missense hotspot mutants R248H:16.3 nM, missense hotspot mutants R273H:3.2 nM, missense hotspot mutants R175H:8.3 nM, KPFLC cells (overexpressing human WT):26.5 nM, Panc05.04 cells:13 nM
In vivo	We conducted a Phase I clinical trial of H3B-8800, an oral small molecule compound that binds splicing factor 3B1 (SF3B1), in patients with MDS, CMML or AML. Of the 84 patients enrolled in the trial (42 MDS, 4 CMML and 38 AML), 62 were dependent on red blood cell (RBC) transfusions at enrollment. The dose-escalation cohort examined two once-daily dosing regimens: regimen I (5 days on/9 days off, study dose range 1-40 mg, n=65) and regimen II (21 days on/7 days off, 7-20 mg, n=19); 27 patients were treated for ≥180 days. The most common treatment-related emergent adverse events included diarrhea, nausea, fatigue, and vomiting. No complete or partial responses meeting IWG criteria were observed; however, RBC transfusion free intervals of more than 56 days were observed in nine patients who were transfusion dependent at enrollment (15%). Five of 15 MDS patients with missense SF3B1 mutations experienced RBC transfusion independence (TI). Increased expression of the pre-treatment target of splicing transmembrane protein 14C (TMEM14C) was observed in MDS patients experiencing RBC TI.

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 | 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

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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.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc