αβ-Tubulin-IN-1

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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

CAS No. : 2478584-74-4

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

αβ-Tubulin^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A2780/Taxol	IC₅₀	13.1 nM Compound: 12b	Cytotoxicity in human A2780T assessed as inhibition in cell growth measured after 24 hrs by MTT assay Cytotoxicity in human A2780T assessed as inhibition in cell growth measured after 24 hrs by MTT assay	[PMID: 35084853]
A2780S	IC₅₀	16.4 nM Compound: 12b	Cytotoxicity in human A2780S assessed as inhibition in cell growth measured after 24 hrs by MTT assay Cytotoxicity in human A2780S assessed as inhibition in cell growth measured after 24 hrs by MTT assay	[PMID: 35084853]
A2780S	IC₅₀	8 nM Compound: 12b	Antiproliferative activity against human A2780S cells assessed as reduction in cell viability measured after 24 hrs by MTT assay Antiproliferative activity against human A2780S cells assessed as reduction in cell viability measured after 24 hrs by MTT assay	[PMID: 35084853]
A549	IC₅₀	60.1 nM Compound: 12b	Cytotoxicity in human A549 assessed as inhibition in cell growth measured after 24 hrs by MTT assay Cytotoxicity in human A549 assessed as inhibition in cell growth measured after 24 hrs by MTT assay	[PMID: 35084853]
A549/TR	IC₅₀	63.8 nM Compound: 12b	Cytotoxicity in human A549T assessed as inhibition in cell growth measured after 24 hrs by MTT assay Cytotoxicity in human A549T assessed as inhibition in cell growth measured after 24 hrs by MTT assay	[PMID: 35084853]
HeLa	IC₅₀	5 nM Compound: 12b	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 24 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 24 hrs by MTT assay	[PMID: 35084853]
MCF7	IC₅₀	11.3 nM Compound: 12b	Cytotoxicity in human MCF7 assessed as inhibition in cell growth measured after 24 hrs by MTT assay Cytotoxicity in human MCF7 assessed as inhibition in cell growth measured after 24 hrs by MTT assay	[PMID: 35084853]
MCF7	IC₅₀	9 nM Compound: 12b	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay	[PMID: 35084853]
NCI/ADR-RES	IC₅₀	13.5 nM Compound: 12b	Cytotoxicity in human NCI-ADR-RES assessed as inhibition in cell growth measured after 24 hrs by MTT assay Cytotoxicity in human NCI-ADR-RES assessed as inhibition in cell growth measured after 24 hrs by MTT assay	[PMID: 35084853]
NCI-H460	IC₅₀	14 nM Compound: 12b	Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay	[PMID: 35084853]
Raji	IC₅₀	13 nM Compound: 12b	Antiproliferative activity against human Raji cells assessed as reduction in cell viability measured after 24 hrs by MTT assay Antiproliferative activity against human Raji cells assessed as reduction in cell viability measured after 24 hrs by MTT assay	[PMID: 35084853]

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.

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
T_1/2 (h)	3.57±1.10	4.42±1.90
CL (L/h/kg)	1.52±0.39	5.06±1.70
V_ss (L/kg)	8.08±4.19	35.26±25.76
AUC_0-∞ (µg/mL·h)	3448.81±782.66	1058.74±285.62
C_max (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.

2478584-74-4

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

Handling Instructions (2659 KB)

References

[1]. Li Y, et al. Structure-Based Design and Synthesis of N-Substituted 3-Amino-β-Carboline Derivatives as Potent αβ-Tubulin Degradation Agents. J Med Chem. 2022 Feb 10;65(3):2675-2693. [Content Brief]

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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