Art. -Nr.: HY-138008

WX-132-18B

WX-132-18B is a tubulin inhibitor with an IC₅₀ of 0.45-0.99 nM. WX-132-18B selectively binds to the colchicine-binding site on tubulin, reduces microtubule content via depolymerization, and inhibits tubulin polymerization. WX-132-18B induces tumor cell cycle arrest, apoptosis and changes in nuclear membrane permeability, and decreases mitochondrial membrane potential. WX-132-18B exhibits antiproliferative activity against endothelial cells and human tumor cells, and inhibits the proliferation and growth of xenograft tumors in mice. WX-132-18B can be used in research related to sarcoma, non-small cell lung cancer, gastric cancer and breast cancer.

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CAS. Nr.: 1415262-07-5
Formel: C₁₈H₁₆N₄O₂
Molecular Weight:320.35

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

WX-132-18B Chemical Structure

CAS. Nr.: 1415262-07-5

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

β-Tubulin

0.47 μM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
786-0	GI₅₀	3.46 nM Compound: 2	Cytotoxicity against human 786-0 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human 786-0 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
A498	GI₅₀	0.376 nM Compound: 2	Cytotoxicity against human A498 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human A498 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
A549	GI₅₀	0.0032 μM Compound: 5f	Cytotoxicity against human A549 cells by SRB assay Cytotoxicity against human A549 cells by SRB assay	[PMID: 24502232]
A549	GI₅₀	0.588 nM Compound: 2	Cytotoxicity against human A549 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human A549 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
ACHN	GI₅₀	0.926 nM Compound: 2	Cytotoxicity against human ACHN cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human ACHN cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
BT-549	GI₅₀	2.1 nM Compound: 2	Cytotoxicity against human BT549 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human BT549 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
CAKI-1	GI₅₀	0.497 nM Compound: 2	Cytotoxicity against human Caki1 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human Caki1 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
CCRF-CEM	GI₅₀	0.551 nM Compound: 2	Cytotoxicity against human CCRF-CEM cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human CCRF-CEM cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
COLO 205	GI₅₀	0.322 nM Compound: 2	Cytotoxicity against human COLO205 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human COLO205 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
DU-145	GI₅₀	0.0019 μM Compound: 5f	Cytotoxicity against human DU145 cells by SRB assay Cytotoxicity against human DU145 cells by SRB assay	[PMID: 24502232]
DU-145	GI₅₀	0.409 nM Compound: 2	Cytotoxicity against human DU145 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human DU145 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
EKVX	GI₅₀	0.632 nM Compound: 2	Cytotoxicity against human EKVX cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human EKVX cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
HCC 2998	GI₅₀	0.371 nM Compound: 2	Cytotoxicity against human HCC2998 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human HCC2998 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
HCT-116	GI₅₀	0.369 nM Compound: 2	Cytotoxicity against human HCT116 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human HCT116 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
HCT-15	GI₅₀	0.413 nM Compound: 2	Cytotoxicity against human HCT15 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human HCT15 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
HL-60(TB)	GI₅₀	0.361 nM Compound: 2	Cytotoxicity against human HL-60(TB) cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human HL-60(TB) cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
HOP-62	GI₅₀	0.69 nM Compound: 2	Cytotoxicity against human HOP62 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human HOP62 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
HOP-92	GI₅₀	>100 nM Compound: 2	Cytotoxicity against human HOP92 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human HOP92 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
Hs-578T	GI₅₀	0.601 nM Compound: 2	Cytotoxicity against human Hs 578T cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human Hs 578T cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
HT-29	GI₅₀	0.307 nM Compound: 2	Cytotoxicity against human HT-29 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human HT-29 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
IGROV-1	GI₅₀	0.83 nM Compound: 2	Cytotoxicity against human IGROV1 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human IGROV1 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
K562	GI₅₀	0.359 nM Compound: 2	Cytotoxicity against human K562 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human K562 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
KB	GI₅₀	0.0023 μM Compound: 5f	Cytotoxicity against human KB cells by SRB assay Cytotoxicity against human KB cells by SRB assay	[PMID: 24502232]
KM12	GI₅₀	0.353 nM Compound: 2	Cytotoxicity against human KM12 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human KM12 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
LOX IMVI	GI₅₀	0.526 nM Compound: 2	Cytotoxicity against human LOXIMVI cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human LOXIMVI cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
M14	GI₅₀	0.336 nM Compound: 2	Cytotoxicity against human M14 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human M14 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
Malme-3M	GI₅₀	>100 nM Compound: 2	Cytotoxicity against human MALME-3M cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human MALME-3M cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
MCF7	GI₅₀	0.363 nM Compound: 2	Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
MDA-MB-231	GI₅₀	0.914 nM Compound: 2	Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
MDA-MB-435	GI₅₀	0.208 nM Compound: 2	Cytotoxicity against human MDA-MB-435 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human MDA-MB-435 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
MDA-MB-468	GI₅₀	0.415 nM Compound: 2	Cytotoxicity against human MDA-MB-468 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human MDA-MB-468 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
MOLT-4	GI₅₀	0.605 nM Compound: 2	Cytotoxicity against human MOLT4 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human MOLT4 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
NCI/ADR-RES	GI₅₀	0.301 nM Compound: 2	Cytotoxicity against human NCI-ADR-RES cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human NCI-ADR-RES cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
NCI-H226	GI₅₀	3.03 nM Compound: 2	Cytotoxicity against human NCI-H226 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human NCI-H226 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
NCI-H23	GI₅₀	0.458 nM Compound: 2	Cytotoxicity against human NCI-H23 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human NCI-H23 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
NCI-H322M	GI₅₀	0.904 nM Compound: 2	Cytotoxicity against human NCI-H322M cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human NCI-H322M cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
NCI-H460	GI₅₀	0.397 nM Compound: 2	Cytotoxicity against human NCI-H460 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human NCI-H460 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
NCI-H522	GI₅₀	0.294 nM Compound: 2	Cytotoxicity against human NCI-H522 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human NCI-H522 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
OVCAR-3	GI₅₀	0.266 nM Compound: 2	Cytotoxicity against human OVCAR3 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human OVCAR3 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
OVCAR-4	GI₅₀	2.43 nM Compound: 2	Cytotoxicity against human OVCAR4 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human OVCAR4 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
OVCAR-5	GI₅₀	>100 nM Compound: 2	Cytotoxicity against human OVCAR5 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human OVCAR5 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
OVCAR-8	GI₅₀	0.524 nM Compound: 2	Cytotoxicity against human OVCAR8 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human OVCAR8 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
PC-3	GI₅₀	0.636 nM Compound: 2	Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
RPMI-8226	GI₅₀	0.603 nM Compound: 2	Cytotoxicity against human RPMI8226 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human RPMI8226 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
RXF 393	GI₅₀	0.246 nM Compound: 2	Cytotoxicity against human RXF393 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human RXF393 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
SF-268	GI₅₀	0.788 nM Compound: 2	Cytotoxicity against human SF268 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human SF268 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
SF-295	GI₅₀	0.318 nM Compound: 2	Cytotoxicity against human SF295 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human SF295 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
SF-539	GI₅₀	0.298 nM Compound: 2	Cytotoxicity against human SF539 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human SF539 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
SK-MEL-28	GI₅₀	>100 nM Compound: 2	Cytotoxicity against human SK-MEL-28 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human SK-MEL-28 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
SK-MEL-5	GI₅₀	0.4 nM Compound: 2	Cytotoxicity against human SK-MEL-5 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human SK-MEL-5 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
SK-OV-3	GI₅₀	0.409 nM Compound: 2	Cytotoxicity against human SKOV3 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human SKOV3 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
SN12C	GI₅₀	1.01 nM Compound: 2	Cytotoxicity against human SN12C cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human SN12C cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
SNB-19	GI₅₀	0.655 nM Compound: 2	Cytotoxicity against human SNB19 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human SNB19 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
SNB-75	GI₅₀	0.36 nM Compound: 2	Cytotoxicity against human SNB75 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human SNB75 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
SR	GI₅₀	0.301 nM Compound: 2	Cytotoxicity against human SR cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human SR cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
SW-620	GI₅₀	0.487 nM Compound: 2	Cytotoxicity against human SW620 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human SW620 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
TK-10	GI₅₀	>100 nM Compound: 2	Cytotoxicity against human TK10 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human TK10 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
U-251	GI₅₀	0.437 nM Compound: 2	Cytotoxicity against human U251 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human U251 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
UACC-257	GI₅₀	>100 nM Compound: 2	Cytotoxicity against human UACC257 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human UACC257 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
UACC-62	GI₅₀	0.432 nM Compound: 2	Cytotoxicity against human UACC62 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human UACC62 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]
UO-31	GI₅₀	10 nM Compound: 2	Cytotoxicity against human UO31 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human UO31 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 28653846]

In Vitro

WX-132-18B (72 h) potently inhibits the proliferation of HepG2, HeLa, A549, H460, BGC-823, MX-1, taxol-resistant MX-1/T, and HUVEC cells with IC₅₀ values ranging from 0.45 to 0.99 nM^[1].
WX-132-18B (1-10 nM; 24 h) reduces tubulin content and altering tubulin morphology with EC₅₀ values ranging from 2.99 to 9.43 nM^[1].
WX-132-18B (0.1-10 μM; 45 min pre-incubation with tubulin, 45 min incubation with colchicine) competitively binds to the colchicine-binding site on tubulin with an IC₅₀ of 0.47 μM^[1].
WX-132-18B (1-10 nM; 24-48 h) potently arrests A549 cells at the G2/M phase of the cell cycle within 24 h, induces concentration-dependent apoptosis in A549 cells after 48 h, and triggers concentration-dependent cytotoxicity in HepG2 cells at 24 h by increasing nuclear membrane permeability while reducing manganese superoxide dismutase levels and mitochondrial membrane potential^[1].
WX-132-18B (0.03-3 μM; per manufacturer instructions) exhibits high target selectivity, with no significant effect on 21 screened tumor-related signaling pathways and only weak, non-specific DNA damage (Rad51 foci induction) at high concentrations^[1].
WX-132-18B (compound 2) displays broad-spectrum and ultra-potent antiproliferative activity with low-to-subnanomolar GI₅₀ values across most NCI-60 human tumor cell lines, although its potency is decreased in HOP-92, MALME-3M, SK-MEL-28, UACC-257, OVCAR-5, and TK-10 cells. It also strongly inhibits the growth of A549, KB, and KB-VIN cells with GI₅₀ values of 2.20-3.20 nM^[2].
WX-132-18B (15 min preincubation; 20 min incubation with GTP) inhibits purified tubulin polymerization with an IC₅₀ of 0.77 μM^[2].

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

Cell Cycle Analysis^[1]

Cell Line:

A549
Concentration:

1, 3, 10 nM
Incubation Time:

24 h
Result:

Induced cell cycle arrest at the G2/M phase in a concentration-dependent manner.
Resulted in 74.77% of cells in the G2/M phase when treated with 3 nM WX-132-18B, compared to 8.68% in the control group.

Apoptosis Analysis^[1]

Cell Line:

A549
Concentration:

1, 3, 10 nM
Incubation Time:

48 h
Result:

Induced A549 cell apoptosis in a concentration-dependent manner.
Produced an apoptotic effect equivalent to that of control microtubule inhibitors (300 nM Colchicine (HY-16569), 300 nM Vincristine (HY-N0488A), 100 nM taxol) when treated with 3 nM WX-132-18B, with significant increases in both early and late apoptotic cell populations.

Cell Cytotoxicity Assay^[1]

Cell Line:

HepG2
Concentration:

3 nM
Incubation Time:

24 h
Result:

Induced concentration-dependent cytotoxic effects including reduced cell count, reduced nuclear size, increased NMP, reduced MnSOD levels, and reduced MMP.
Produced a cytotoxic profile similar to 300 nM Colchicine, 300 nM Vincristine, and 100 nM taxol at 3 nM, with stronger effects on MnSOD and MMP reduction, and weaker effects on NMP increase, compared to taxol or vincristine.

In Vivo

WX-132-18B (0.25-1.0 mg/kg; i.p.; twice a week; 3 weeks) dose-dependently inhibits sarcoma S180 xenograft growth in KM mice^[1].
WX-132-18B (0.25-1.0 mg/kg; i.p.; twice a week; 3 weeks) dose-dependently inhibits BGC-823 human gastric cancer xenograft growth in nude mice via inducing apoptosis, inhibiting cell proliferation, and suppressing angiogenesis^[1].
WX-132-18B (0.25-1.0 mg/kg; i.p.; once every 5 days; 3 weeks) dose-dependently inhibits H460 human non-small cell lung cancer xenograft growth in nude mice^[1].
WX-132-18B (compound 2) (0.25-1.0 mg/kg; i.v.; every 5 days; 3 weeks) exhibits dose-dependent in vivo antitumor activity against NCI-H460 xenografts^[2].

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

Animal Model:

Kunming (KM) mice (6- to 8-week-old; subcutaneous S180 sarcoma model)^[1]
Dosage:

0.25 mg/kg; 0.5 mg/kg; 1.0 mg/kg
Administration:

i.p.; twice a week; 3 weeks
Result:

Induced 70.06% inhibition of tumor volume at 1.0 mg/kg.
Induced 72.62% inhibition of tumor weight at 1.0 mg/kg.
Inhibited tumor growth in a dose-dependent manner.

Animal Model:

Nude mice (Nu/Nu) (8-week-old; subcutaneous H460 non-small cell lung cancer model)^[1]
Dosage:

0.25 mg/kg; 0.5 mg/kg; 1.0 mg/kg
Administration:

i.p.; once every 5 days; 3 weeks
Result:

Induced 68.70% inhibition of tumor volume at 1.0 mg/kg.
Induced 61.90% inhibition of tumor weight at 1.0 mg/kg.
Exhibited anti-tumor effect comparable to that of 15 mg/kg taxol at 1.0 mg/kg.

Animal Model:

Nude mice (Nu/Nu) (8-week-old; subcutaneous BGC-823 gastric cancer model)^[1]
Dosage:

0.25 mg/kg; 0.5 mg/kg; 1.0 mg/kg
Administration:

i.p.; twice a week; 3 weeks
Result:

Induced 76.06% inhibition of tumor volume at 1.0 mg/kg.
Induced 77.32% inhibition of tumor weight at 1.0 mg/kg.
Caused shrunken, structurally incomplete nuclei in treated tumor tissues versus enlarged, deeply stained nuclei in controls.
Increased caspase 3 expression, reduced Ki67 expression, and reduced CD31 expression in a dose-dependent manner.

Animal Model:

Balb/c-nu nude mice (female, 6 weeks old)^[2]
Dosage:

0.25 mg/kg; 0.5 mg/kg; 1.0 mg/kg
Administration:

i.v.; every 5 days; 3 weeks
Result:

Reduced mean tumor weight and increased tumor growth inhibition in a dose‑dependent manner: 17.8% (2.23 g) at 0.25 mg/kg, 36.8% (1.72 g) at 0.5 mg/kg, and 61.9% (1.03 g) at 1.0 mg/kg.
Reduced vessel size and number via CD31 staining.
Increased cleaved caspase-3 staining, indicating apoptosis.
Decreased Ki67 staining, indicating reduced tumor cell proliferation.

Related Protocols :

Chemical Information

CAS. Nr. 1415262-07-5
Molecular Weight 320.35
Formel C₁₈H₁₆N₄O₂
SMILES

O=C1NC2=CC(OC)=CC=C2N(C=3N=C(N=C4C=CC=CC43)C)C1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Guan F, et al. WX-132-18B, a novel microtubule inhibitor, exhibits promising anti-tumor effects. Oncotarget. 2017 May 9;8(42):71782-71796. [Content Brief]

[2]. Cui MT, et al. In Vivo and Mechanistic Studies on Antitumor Lead 7-Methoxy-4-(2-methylquinazolin-4-yl)-3,4-dihydroquinoxalin-2(1H)-one and Its Modification as a Novel Class of Tubulin-Binding Tumor-Vascular Disrupting Agents. J Med Chem. 2017;60(13):5586-5598. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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WX-132-18B