Tubulin degrader 1

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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.

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Tubulin degrader 1 Chemical Structure

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Biological Activity
Purity & Documentation
References
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Description

Cellular Effect

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]
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]
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]
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]

In Vitro

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.

In Vivo

Tubulin degrader 1 (10-30 mg/kg, i.v., every two days for 6-9 doses) has antitumor activity in A2780S and A2780T xenograft models^[1].

Pharmacokinetic Analysis in Male Sprague–Dawley Rat Model^[1]

Route	Dose (mg/kg)	T_1/2 (h)	T_max (h)	CL_obs (L/h/kg)	V_ss (L/kg)	AUC_0-t (μg/mL*h)	C_max (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

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

Molecular Weight

345.40

Formula

C₂₀H₁₉N₅O

SMILES

COC1=CC=CC(C2=CC(NCC3=CC4=C(NC=C4)C=C3)=NC(N)=N2)=C1

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

Handling Instructions (2659 KB)

References

[1]. Zhang C, et al. Structure-based design and synthesis of BML284 derivatives: A novel class of colchicine-site noncovalent tubulin degradation agents. Eur J Med Chem. 2024 Feb 27;268:116265. [Content Brief]