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Cat. No.: HY-116068

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DW532

DW532 is a dual inhibitor of tubulin and tyrosine kinase, with IC₅₀ values of 4.9 μM and 5.5 μM against EGFR and VEGFR2, respectively, and a K_D of 3.6 μM for tubulin. DW532 induces cell cycle arrest at the G₂/M phase, triggers cell apoptosis via caspase-related pathways, and inhibits angiogenesis. DW532 can be used for research related to cancers (e.g., breast cancer).

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CAS No.: 1267949-42-7
화학식: C₁₆H₁₂O₆
분자량:300.27

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

DW532 Chemical Structure

CAS No.: 1267949-42-7

Amount: USD 0.00

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Use of MCE Products

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target^[1]

VEGFR2

5.5 μM (IC₅₀)

EGFR

4.9 μM (IC₅₀)

C-src

8.6 μM (IC₅₀)

All EGFR Isoforms :

All VEGFR Isoforms :

All Src Isoforms :

In Vitro

DW532 (1-10 μM; 2 h) dose-dependently inhibits ligand-induced VEGFR2 activation and its downstream signaling pathways in HUVECs, as well as EGFR activation and its downstream signaling pathways in A431 human epithelial cancer cells^[1].
DW532 (10-40 μM; 30 min) is a microtubule destabilizer that inhibits tubulin polymerization in vitro in a dose-dependent manner^[1].
DW532 (0.1-10 μM; 12 h) dose-dependently inhibits tubulin polymerization in human breast cancer MDA-MB-468 cells, reduces the level of polymerized tubulin and increases the level of soluble tubulin^[1].
DW532 (10 μM; 6 h) disrupts the microtubule network in human lung cancer A549 cells and induces diffuse tubulin staining, which is consistent with the characteristics of microtubule destabilization^[1].
DW532 (72 h) potently and non-selectively inhibits the proliferation of a panel of 16 human cancer cell lines, with a mean IC₅₀ of 1.82 μM^[1].
DW532 (0.1-10 μM; 6 h) dose-dependently inhibits tube formation in human umbilical vein endothelial cells (HUVECs) in vitro^[1].
DW532 (10 μM; 12 h) disrupts mitotic spindle assembly in human lung cancer A549 cells, induces chromosome dispersion and multipolar spindle formation, and rarely causes the appearance of monopolar spindles^[1].
DW532 (1-10 μM; 24 h) induces G₂/M phase arrest in MDA-MB-468, A549, PC-3, KB, K562 and A431 human cancer cells, accompanied by altered levels of mitosis-related proteins cyclin B1, p-CDK1 and p-H3^[1].
DW532 (0.1-20 μM; 48 h) induces dose-dependent apoptosis in KB, MDA-MB-468 and A431 human cancer cells via a caspase-related mechanism^[1].

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

Western Blot Analysis^[1]

Cell Line:

human umbilical vein endothelial cells (HUVECs), A431 human epithelial cancer cells
Concentration:

1, 5 and 10 μM
Incubation Time:

2 h (pre-incubated prior to 15 min ligand stimulation)
Result:

Dose-dependently inhibited VEGF-induced phosphorylation of VEGFR2 and its downstream target Akt in HUVECs.
Similarly inhibited EGF-induced phosphorylation of EGFR and downstream Akt in A431 cells.

Western Blot Analysis^[1]

Cell Line:

MDA-MB-468 human breast carcinoma cells
Concentration:

0.1, 1 and 10 μM
Incubation Time:

12 h
Result:

Dose-dependently decreased polymerized tubulin in pellets and increased soluble tubulin in supernatants, promoting the transition of cellular tubulin from polymerized to free state.

Immunofluorescence^[1]

Cell Line:

A549 human lung cancer cells
Concentration:

10 μM
Incubation Time:

6 h
Result:

Disrupted the intact, stretched microtubule network seen in untreated cells, resulting in dispersed tubulin staining similar to that induced by the microtubule destabilizer vincristine (VCR).

Immunofluorescence^[1]

Cell Line:

A549 human lung cancer cells
Concentration:

10 μM
Incubation Time:

12 h
Result:

Induced scattered chromosomes in the cytoplasm, formation of multipolar spindles, and a small proportion of monopolar spindles, consistent with traditional microtubule destabilizers.

Apoptosis Analysis^[1]

Cell Line:

KB mouth epidermal carcinoma cells, MDA-MB-468 human breast carcinoma cells, A431 human epithelial carcinoma cells
Concentration:

0.1, 1 and 10 μM (Annexin V/PI); 0.1, 1, 5, 10 and 20 μM (Western Blot)
Incubation Time:

48 h
Result:

Induced dose-dependent apoptosis: ~59.7% of KB cells underwent apoptosis at 1 μM, and ~70% at 10 μM.
Dose-dependently increased cleavage of caspase-3, caspase-9, and PARP, indicating a caspase-related apoptosis mechanism.

Cell Cycle Analysis^[1]

Cell Line:

MDA-MB-468, A549, PC-3, KB, K562, and A431 human cancer cells
Concentration:

1 and 10 μM
Incubation Time:

24 h
Result:

Arrested all six tested cell lines at the G₂/M phase.
Increased levels of mitotic markers cyclin B1 and p-H3, and decreased levels of phosphorylated (inhibitory) CDK1 (Tyr15).

In Vivo

DW532 (0.1-1 nmol per egg; local application) potently inhibits in vivo angiogenesis in the chick chorioallantoic membrane model^[1].

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

Animal Model:

fertilized eggs^[1]
Dosage:

0.1 nmol per egg; 1 nmol per egg
Administration:

local application
Result:

Significantly inhibited neovascularization at both tested doses compared to untreated controls.

Chemical Information

CAS No. 1267949-42-7
분자량 300.27
화학식 C₁₆H₁₂O₆
SMILES

O=C1OC=2C(O)=C(O)C=CC2C(=C1)C=3C=CC(OC)=C(O)C3
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Handling Instructions (2659 KB)

References

[1]. Peng T, et al. Identification of DW532 as a novel anti-tumor agent targeting both kinases and tubulin. Acta pharmacologica Sinica. 2014 Jul;35(7):916-28. [Content Brief]

Calculators

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

MOQ

Minimum order quantity

100 mg

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Other size

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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

상품명:
Cat. No.:
수량:
MCE Japan Authorized Agent:

상품명:
CAS No.:
Species:
Purity:
수량:

DW532

All EGFR Isoforms

All VEGFR Isoforms

All Src Isoforms