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.
For research use only. We do not sell to patients.
- CAS No.: 1415262-07-5
- Formula: C18H16N4O2
- Molecular Weight:320.35
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
β-Tubulin 0.47 μM (IC50) |
|
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] |
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 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.
-
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 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.
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.
Chemical Information
-
CAS No. 1415262-07-5
-
Molecular Weight 320.35
-
Formula C18H16N4O2
-
SMILES
O=C1NC2=CC(OC)=CC=C2N(C=3N=C(N=C4C=CC=CC43)C)C1
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Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)