H3B-8800

Cat. No.: HY-111517: FAQs
Data Sheet Handling Instructions

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H3B-8800 is a potent and orally active SF3B splicing modulator. H3B-8800 direct interaction with the SF3b complex and shows anti-cancer activity. H3B-8800 has the potential for the research of acute myeloid leukemia (AML) with SF3B1 mutant.

For research use only. We do not sell to patients.

H3B-8800 Chemical Structure

CAS No. : 1825302-42-8

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

SF3B splicing^[1]

In Vitro

H3B-8800 (0.1-10000 nM; 72 h) inhibits cell growth in SF3B1-mutant cell line Panc05.04 cells^[1].
H3B-8800 (0.1-10000 nM; 24 h) induces apoptosis in SF3B1-mutant cell line Panc05.04 cells in a dose-dependent manner^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis^[1]

Cell Line:	SF3B1-mutant cell line Panc05.04 cells
Concentration:	0.1,1, 10, 100, 1000, 10000 nM
Incubation Time:	24 h
Result:	Induced apoptosis by increased caspase-3/7 cleavage in a dose-dependent manner.

In Vivo

H3B-8800 (2, 4 mg/kg; p.o.; daily) shows anti tumor activity in AML derived xenografts (PDXs) with a mutation in SF3B1^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	6-8 weeks, female NSG or CB17-SCID mice (K562 cells with SF3B1^WT or SF3B1^K700E)^[1]
Dosage:	2, 4 mg/kg
Administration:	P.o.; daily
Result:	Resulted in antileukemic efficacy and splicing modulation in mice bearing AML patient-derived xenografts (PDXs) with a mutation in SF3B1 but had little effect in mice bearing SF3B1WT AML PDXs, significantly reduced leukemic burden relative in SF3B1K700E PDX.

Molecular Weight

555.71

Formula

C₃₁H₄₅N₃O₆

CAS No.

1825302-42-8

Appearance

Solid

Color

Yellow to orange

SMILES

O=C(N1CCN(C)CC1)O[C@H]([C@](C)(O)CC[C@@H](O)C2)/C=C/[C@H](C)[C@H](OC2=O)/C(C)=C/C=C/[C@@H](C)C3=NC=CC=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (179.95 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.7995 mL	8.9975 mL	17.9950 mL
5 mM	0.3599 mL	1.7995 mL	3.5990 mL
10 mM	0.1799 mL	0.8997 mL	1.7995 mL

View the 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.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Seiler M, et al. H3B-8800, an orally available small-molecule splicing modulator, induces lethality in spliceosome-mutant cancers. Nat Med. 2018 May;24(4):497-504. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7995 mL	8.9975 mL	17.9950 mL	44.9875 mL
	5 mM	0.3599 mL	1.7995 mL	3.5990 mL	8.9975 mL
	10 mM	0.1799 mL	0.8997 mL	1.7995 mL	4.4987 mL
	15 mM	0.1200 mL	0.5998 mL	1.1997 mL	2.9992 mL
	20 mM	0.0900 mL	0.4499 mL	0.8997 mL	2.2494 mL
	25 mM	0.0720 mL	0.3599 mL	0.7198 mL	1.7995 mL
	30 mM	0.0600 mL	0.2999 mL	0.5998 mL	1.4996 mL
	40 mM	0.0450 mL	0.2249 mL	0.4499 mL	1.1247 mL
	50 mM	0.0360 mL	0.1799 mL	0.3599 mL	0.8997 mL
	60 mM	0.0300 mL	0.1500 mL	0.2999 mL	0.7498 mL
	80 mM	0.0225 mL	0.1125 mL	0.2249 mL	0.5623 mL
	100 mM	0.0180 mL	0.0900 mL	0.1799 mL	0.4499 mL

H3B-8800 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

H3B-88001825302-42-8DNA/RNA SynthesisApoptosisacute myeloid leukemiaapoptosiscaspase-3/7Panc05.04 cellsSF3B1K700EanticancerInhibitorinhibitorinhibit

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