Tubulin degrader 1
Tubulin degrader 1 (Compound 5i) is a BML284 (HY-19987) derivative that is an orally active colchicine-site noncovalent tubulin degradation agent with IC50 values ranging from 0.02 to 0.05 μM against the five tumor cell lines (Hela, HCT116, MCF-7, K562 and Molm-13). Tubulin degrader 1 has antiproliferative activity that effectively suppressed tumor growth.
For research use only. We do not sell to patients.
- Formula: C20H19N5O
- Molecular Weight:345.40
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A2780/Taxol | IC50 |
16 nM
Compound: 5i
|
Antiproliferative activity against human A2780T cells assessed as reduction in cell viability measured after 72 hrs
Antiproliferative activity against human A2780T cells assessed as reduction in cell viability measured after 72 hrs
|
[PMID: 38430854] |
| A2780S | IC50 |
18 nM
Compound: 5i
|
Antiproliferative activity against human A2780S cells assessed as reduction in cell viability measured after 72 hrs
Antiproliferative activity against human A2780S cells assessed as reduction in cell viability measured after 72 hrs
|
[PMID: 38430854] |
| A549 | IC50 |
34 nM
Compound: 5i
|
Antiproliferative activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs
Antiproliferative activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs
|
[PMID: 38430854] |
| A549/TR | IC50 |
37 nM
Compound: 5i
|
Antiproliferative activity against paclitaxel resistant human A549T cells assessed as reduction in cell viability measured after 72 hrs
Antiproliferative activity against paclitaxel resistant human A549T cells assessed as reduction in cell viability measured after 72 hrs
|
[PMID: 38430854] |
| HCT-116 | IC50 |
0.03 μM
Compound: 5i
|
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability measured after 72 hrs
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability measured after 72 hrs
|
[PMID: 38430854] |
| HeLa | IC50 |
0.05 μM
Compound: 5i
|
Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs
Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs
|
[PMID: 38430854] |
| HUVEC | IC50 |
623 nM
Compound: 5i
|
Antivascular activity against human HUVEC cells assessed as inhibition of capillary tube formation incubated for 24 hrs by microscopy based analysis
Antivascular activity against human HUVEC cells assessed as inhibition of capillary tube formation incubated for 24 hrs by microscopy based analysis
|
[PMID: 38430854] |
| K562 | IC50 |
0.03 μM
Compound: 5i
|
Antiproliferative activity against human K562 cells assessed as reduction in cell viability measured after 72 hrs
Antiproliferative activity against human K562 cells assessed as reduction in cell viability measured after 72 hrs
|
[PMID: 38430854] |
| MCF7 | IC50 |
20 nM
Compound: 5i
|
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs
|
[PMID: 38430854] |
| MOLM-13 | IC50 |
0.02 μM
Compound: 5i
|
Antiproliferative activity against human MOLM-13 cells assessed as reduction in cell viability measured after 72 hrs
Antiproliferative activity against human MOLM-13 cells assessed as reduction in cell viability measured after 72 hrs
|
[PMID: 38430854] |
| NCI/ADR-RES | IC50 |
32 nM
Compound: 5i
|
Antiproliferative activity against human MCF7ADR cells assessed as reduction in cell viability measured after 72 hrs
Antiproliferative activity against human MCF7ADR cells assessed as reduction in cell viability measured after 72 hrs
|
[PMID: 38430854] |
Tubulin degrader 1 (0.2-25 μM, 24 h) exerts its antiproliferative activity by directly binding to the colchicine-site in Hela cells[1].
Tubulin degrader 1 (0-300 nM, 24 h) can cause apparent G2/M phase cell cycle arrest and cell apoptosis in A2780S and A2780T cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pharmacokinetic Analysis in Male Sprague–Dawley Rat Model[1]
| Route | Dose (mg/kg) | T1/2 (h) | Tmax (h) | CLobs (L/h/kg) | Vss (L/kg) | AUC0-t (μg/mL*h) | Cmax (μg/mL) | F (%) |
| i.v. | 10 | 1.93 | 0.08 | 2.55 | 7.43 | 4266.53 | 2885.77 | - |
| p.o. | 10 | 5.94 | 3.67 | 18.86 | 154.68 | 446.77 | 77.92 | 10.47 |