2. Apoptosis Epigenetics
  3. Apoptosis SF3B1
  4. H3B-8800

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

H3B-8800 Chemical Structure

CAS No. : 1825302-42-8

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5 mg USD 950 In-stock
10 mg USD 1520 In-stock
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Based on 1 publication(s) in Google Scholar

H3B-8800 Related Antibodies

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Description

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[1].

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.

H3B-8800 Related Antibodies

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 SF3B1WT or SF3B1K700E)[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.
Appearance

Solid

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
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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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Purity & Documentation
References

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.

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
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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-88001825302-42-8ApoptosisSF3B1Splicing Factor 3b Subunit 1acute myeloid leukemiaapoptosiscaspase-3/7Panc05.04 cellsSF3B1K700EanticancerInhibitorinhibitorinhibit

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