2. Stem Cell/Wnt
  3. β-catenin
  4. ZW4864 free base

ZW4864 (free base) is an orally active and selective β catenin/B-Cell lymphoma 9 protein−protein interaction (β catenin/BCL9 PPI) inhibitor. ZW4864 (free base) inhibits β catenin/BCL9 PPI with a Ki value of 0.76 μM and an IC50 value of 0.87 μM.

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ZW4864 free base Chemical Structure

ZW4864 free base Chemical Structure

CAS No. : 2632259-92-6

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 550 In-stock
Solution
10 mM * 1 mL in DMSO USD 550 In-stock
Solid
5 mg USD 500 In-stock
10 mg USD 850 In-stock
25 mg USD 1800 In-stock
50 mg USD 3000 In-stock
100 mg USD 4600 In-stock
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Based on 1 publication(s) in Google Scholar

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ZW4864 free base Related Antibodies

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Description

ZW4864 (free base) is an orally active and selective β catenin/B-Cell lymphoma 9 protein−protein interaction (β catenin/BCL9 PPI) inhibitor. ZW4864 (free base) inhibits β catenin/BCL9 PPI with a Ki value of 0.76 μM and an IC50 value of 0.87 μM[1].

IC50 & Target

IC50: 0.87 μM (β catenin/BCL9 PPI)[1].
Ki: 0.76 μM (β catenin/BCL9 PPI)[1]
In Vitro

ZW4864 (10~40 μM; 24 hours; SW480 and MBA-MD-231 cells) (free base) decreases the expression levels of Axin2 and cyclin D1 proteins[1].
ZW4864 (10~40 μM; 72 hours; MDA-MB231, MCF10A and MDA-MB-468 cells) (free base) selectively triggeres rapid apoptosis of triple-negative breast cancer cells with hyperactive β-catenin signaling while sparing normal mammary epithelial MCF10A cells[1].
ZW4864 (10~40 μM; 24 hours; SW480 and MBA-MD-231 cells) (free base) suppresses the transcription of β-catenin target genes in a concentration-dependent manner without affecting the expression of HPRT, a house-keeper gene, in both SW480 and Wnt 3a-activated MDA-MB-231 cells[1].
ZW4864 (free base) binds with β-catenin and selectively disrupts the protein−protein interaction (PPI) between B-cell lymphoma 9 (BCL9) and β-catenin while sparing the β-catenin/E-cadherin PPI. ZW4864 (free base) dose-dependently suppresses β-catenin signaling activation, downregulates oncogenic β-catenin target genes, and abrogates invasiveness of β-catenin-dependent cancer cells. ZW4864 (free base) suppresses TOPFlash luciferase activities in β-catenin expressing HEK293 cells in a dose-dependent manner with an IC50 of 11 μM. ZW4864 (free base) also dose-dependently suppresses the TOPFlash luciferase activities in SW480 and Wnt 3a-activated MDA-MB-468 cells with the IC50s of 7.0 and 6.3 μM, respectively. ZW4864 (free base) selectively suppresses transactivation of β-catenin signaling[1].

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

ZW4864 free base Related Antibodies

Western Blot Analysis[1]

Cell Line: SW480 and MBA-MD-231 cells
Concentration: 10~40 μM
Incubation Time: 24 hours
Result: Decreased the expression levels of Axin2 and cyclin D1 proteins.

Apoptosis Analysis[1]

Cell Line: MDA-MB231, MCF10A and MDA-MB-468 cells
Concentration: 10~40 μM
Incubation Time: 72 hours
Result: Selectively triggered rapid apoptosis of triple-negative breast cancer cells with hyperactive β-catenin signaling while sparing normal mammary epithelial MCF10A cells.

RT-PCR[1]

Cell Line: SW480 and MBA-MD-231 cells
Concentration: 10~40 μM
Incubation Time: 24 hours
Result: Suppressed the transcription of β-catenin target genes in a concentration-dependent manner without affecting the expression of HPRT, a house-keeper gene, in both SW480 and Wnt 3a-activated MDA-MB-231 cells.
In Vivo

ZW4864 (20 mg/kg; p.o.) (free base) exhibits good pharmacokinetic properties with an oral bioavailability (F) of 83 %[1].
ZW4864 (90 mg/kg; p.o.) (free base) shows a variation in tumor growth in mice[1].
ZW4864 (free base) shows good pharmacokinetic properties and effectively suppresses β-catenin target gene expression in the patient-derived xenograft mouse model[1].

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

Animal Model: C57BL/6 mice[1]
Dosage: 20 mg/kg (Pharmacokinetic Analysis)
Administration: P.o.
Result: Exhibited good pharmacokinetic properties with an oral bioavailability (F) of 83%.
Animal Model: Mice[1]
Dosage: 90 mg/kg
Administration: P.o.
Result: Showed a variation in tumor growth in mice.
Molecular Weight

570.72

Formula

C33H42N6O3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C([C@H]1CN(C2=CC=CC(OC(C)(C)C(N3CCNCC3)=O)=C2)CCC1)N(C4CC4)CC5=CC=C(C6=CNN=C6)C=C5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (175.22 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7522 mL 8.7609 mL 17.5217 mL
5 mM 0.3504 mL 1.7522 mL 3.5043 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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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 1.7522 mL 8.7609 mL 17.5217 mL 43.8043 mL
5 mM 0.3504 mL 1.7522 mL 3.5043 mL 8.7609 mL
10 mM 0.1752 mL 0.8761 mL 1.7522 mL 4.3804 mL
15 mM 0.1168 mL 0.5841 mL 1.1681 mL 2.9203 mL
20 mM 0.0876 mL 0.4380 mL 0.8761 mL 2.1902 mL
25 mM 0.0701 mL 0.3504 mL 0.7009 mL 1.7522 mL
30 mM 0.0584 mL 0.2920 mL 0.5841 mL 1.4601 mL
40 mM 0.0438 mL 0.2190 mL 0.4380 mL 1.0951 mL
50 mM 0.0350 mL 0.1752 mL 0.3504 mL 0.8761 mL
60 mM 0.0292 mL 0.1460 mL 0.2920 mL 0.7301 mL
80 mM 0.0219 mL 0.1095 mL 0.2190 mL 0.5476 mL
100 mM 0.0175 mL 0.0876 mL 0.1752 mL 0.4380 mL
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ZW4864 free base 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:

ZW48642632259-92-6ZW 4864ZW-4864β-cateninBeta cateninorallyactiveselectiveβ cateninB-CelllymphomaproteininteractionInhibitorinhibitorinhibit

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