2. Apoptosis Cytoskeleton Cell Cycle/DNA Damage
  3. Apoptosis Microtubule/Tubulin
  4. αβ-Tubulin-IN-1

αβ-Tubulin-IN-1 is a potent and orally active αβ-Tubulin inhibitor. αβ-Tubulin-IN-1 induces cell cycle arrest at G2/M and efficient apoptosis. αβ-Tubulin-IN-1 inhibits tumor cell migration and Metastasis. αβ-Tubulin-IN-1 shows significant antitumor efficacy in a dose dependent manner.

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αβ-Tubulin-IN-1 Chemical Structure

αβ-Tubulin-IN-1 Chemical Structure

CAS No. : 2478584-74-4

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αβ-Tubulin-IN-1 Related Antibodies

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Description

αβ-Tubulin-IN-1 is a potent and orally active αβ-Tubulin inhibitor. αβ-Tubulin-IN-1 induces cell cycle arrest at G2/M and efficient apoptosis. αβ-Tubulin-IN-1 inhibits tumor cell migration and Metastasis. αβ-Tubulin-IN-1 shows significant antitumor efficacy in a dose dependent manner[1].

IC50 & Target

αβ-Tubulin[1]
In Vitro

αβ-Tubulin-IN-1 (compound 12 b) (0, 0.5, 1, 5, 10, 50 µM; 16 h) promotes αβ-tubulin degradation in a concentration-dependent manner in Hela and K562 (0-10 µM) cells[1].
αβ-Tubulin-IN-1 exhibits potent cytotoxic activity toward sensitive cells and resistant cells[1].
αβ-Tubulin-IN-1 (0-300 nM; 48 h) induces cell cycle arrest at G2/M and efficient apoptosis in A2780S and A2780T cells[1].
αβ-Tubulin-IN-1 (0, 1.25, 2.5, 5, 10 nM; 24, 48 h) inhibits tumor cell migration and Metastasis with the inhibition rate of 76.21% and 85.07% for 24 , 48 h in human umbilical vein endothelial cells (HUVEC)[1].

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

αβ-Tubulin-IN-1 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: Hela, A2780S, MCF-7, Raji, H460 cells
Concentration: 0-500 nM
Incubation Time: 24 h
Result: Showed anti-proliferative activity with IC50s of 5, 8, 9,13, 14 nM for Hela, A2780S, MCF-7, Raji, H460 cells, respectively.

Western Blot Analysis[1]

Cell Line: HeLa cells
Concentration: 10 µM
Incubation Time: 16 h
Result: Remarkably promoted tubulin degradation by binding to the colchicine site, and the degradation process relied on the ubiquitin−proteasome pathway.

Cell Viability Assay[1]

Cell Line: A2780S, A2780T, A549, A549T, MCF7, MCF7/ADR cells
Concentration:
Incubation Time: 24 h
Result: Exhibited potent cytotoxic activity with IC50s of 16.4, 13.1, 60.1, 63.8, 11.3, 13.5 nM for A2780S, A2780T, A549, A549T, MCF7, MCF7/ADR cells, respectively.

Cell Cycle Analysis[1]

Cell Line: A2780S (PTX-sensitive), A2780T ( PTX-resistant) cells
Concentration: 0, 3, 10, 30, 100, 300 nM
Incubation Time: 48 h
Result: Induced cell cycle arrest at G2/M phase with the the percentages of A2780S and A2780T cells were 55.10%, 72.18% at 100 nM, and 79.54%, 72.89% at 300 nM.

Apoptosis Analysis[1]

Cell Line: A2780S, A2780T cells
Concentration: 0, 3, 10, 30, 100, 300 nM
Incubation Time: 48 h
Result: Induced cell apoptosis with the total numbers of late apoptotic cells were 3.7%, 25.2%, 30.6% at 30,100, and 300 nM, and 5.2% % late apoptotic cells in control.
In Vivo

αβ-Tubulin-IN-1 (5 mg/kg; i.v., p.o.) shows intravenous and oral administration approaches are available in vivo[1].
αβ-Tubulin-IN-1 (10, 20, 40 mg/kg; i.v.; 3 times a week for 2-4 weeks) shows significant antitumor efficacy in a dose dependent manner[1].
Pharmacokinetic Parameters of αβ-Tubulin-IN-1 in rats[1].

route i.v. p.o.
dose (mg/kg) 5 5
T1/2 (h) 3.57±1.10 4.42±1.90
CL (L/h/kg) 1.52±0.39 5.06±1.70
Vss (L/kg) 8.08±4.19 35.26±25.76
AUC0-∞ (µg/mL·h) 3448.81±782.66 1058.74±285.62
Cmax (µg/L) 2601.47±444.20 189.29±119.02
F (%) 30.70
Rats, 5 mg/kg for i.v., 5 mg/kg for p.o.[1].

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

Animal Model: Rats[1]
Dosage: 5 mg/kg
Administration: I.v. or p.o.
Result: Showed oral bioavailability (F=30.70%) with the T1/2 values for intravenous and oral administration approaches are 3.57 h and 4.42 h, respectively.
Animal Model: 5-6weeks female Balb/C and athymic nude mice (A2780S and A2780T Xenograft) Models[1]
Dosage: 10, 20, 40 mg/kg for i.v., 40 mg/kg for p.o.
Administration: I.v.; 3 times a week for 2-4 weeks
Result: Showed significant antitumor efficacy with tumor growth inhibition (TGI) of 66.06%, 71.47% and 92.41% at 10, 20 and 40 mg/kg in A2780S xenograft nude mice model, and 26.94%, 37.2%, 75.73% at 10, 20 and 40 mg/kg in PTX-resistant A2780T xenograft model for i.v. injection, did not show an acceptable antitumor efficacy with 34.93% of TGI at the 40 mg/kg for p.o..
Molecular Weight

409.44

Formula

C25H19N3O3
CAS No.
SMILES

C(N1)(C=NC(NCC2=CC=CC(OC3=CC=C(OCO4)C4=C3)=C2)=C5)=C5C6=C1C=CC=C6
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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αβ-Tubulin-IN-1 Related Classifications

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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.

Keywords:

αβ-Tubulin-IN-12478584-74-4ApoptosisMicrotubule/Tubulinorally activeantitumorapoptosisubiquitin?proteasomeG2/MHeLa cellsXenograft modelmigrationInhibitorinhibitorinhibit

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