1. Cell Cycle/DNA Damage Cytoskeleton
  2. Microtubule/Tubulin
  3. 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.

Tubulin degrader 1 Chemical Structure

Tubulin degrader 1 Chemical Structure

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Description

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[1].

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) 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

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
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Tubulin degrader 1
Cat. No.:
HY-161324
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