IDO/Tubulin-IN-2

Name: IDO/Tubulin-IN-2
Brand: MedChemExpress
SKU: HY-146715

Cat. No.: HY-146715: FAQs
Data Sheet Handling Instructions

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IDO/Tubulin-IN-2 (HT2) is a potent TDO and tubulin inhibitor. IDO/Tubulin-IN-2 also shows potent activity against U87, HepG2, A549, HCT-116, and LO2 cancer cell lines, with IC₅₀ values of 0.43, 0.036, 0.041, 0.095 and 1.04 μM, respectively. IDO/Tubulin-IN-2 remarkably promotes the antitumor activity.

For research use only. We do not sell to patients.

IDO/Tubulin-IN-2 Chemical Structure

CAS No. : 2409479-24-7

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References
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Description

IC₅₀ & Target

TDO, Tubulin^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.041 μM Compound: HT2	Antiproliferative activity against human A549 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay	[PMID: 31830637]
HCT-116	IC₅₀	0.095 μM Compound: HT2	Antiproliferative activity against human HCT116 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay	[PMID: 31830637]
HepG2	IC₅₀	0.036 μM Compound: HT2	Antiproliferative activity against human HepG2 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay	[PMID: 31830637]
L02	IC₅₀	1.04 μM Compound: HT2	Cytotoxicity against human LO2 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay Cytotoxicity against human LO2 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay	[PMID: 31830637]
U-87MG ATCC	IC₅₀	0.43 μM Compound: HT2	Antiproliferative activity against human U87 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human U87 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay	[PMID: 31830637]

In Vitro

IDO/Tubulin-IN-2 (HT2) (0-50 μM, 4 h) shows potent cytotoxicity with IC₅₀ values between 0.036 and 0.43 μM against cancer cell lines^[1].
IDO/Tubulin-IN-2 (0.1 μM, 24 h) arrests the HepG2 cells cycle mainly at the G2 phase^[1].
IDO/Tubulin-IN-2 (0.1 μM, 24 h) can effectively cause cell apoptosis^[1].
IDO/Tubulin-IN-2 (0.1 μM, 24 h) has strongly effects on inducing the proteolytic cleavage of PARP and up-regulating the expression level of caspase-3^[1].
IDO/Tubulin-IN-2 (0.05 μM, 24, 48 and 72 h) markedly decreases mRNA expression level of TDO at a time-dependent manner^[1].
IDO/Tubulin-IN-2 (2 days) can improve T-cell activation and proliferation and enhance immune response^[1].

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

Cell Proliferation Assay

Cell Line:	Human cancer cell lines and non-tumoral cell line^[1]
Concentration:	0-50 μM
Incubation Time:	4 h
Result:	Displayed potent cytotoxicity with IC₅₀ values of 0.43 μM (U87), 0.036 μM (HepG2), 0.041 μM (A549), 0.095 μM (HCT-116), and 1.04 μM (LO2).

Cell Cycle Analysis

Cell Line:	HepG2 cells^[1]
Concentration:	0.1 μM
Incubation Time:	24 h
Result:	Arrested the HepG2 cells cycle mainly at the G2 phase.

Apoptosis Analysis

Cell Line:	HepG2 cells^[1]
Concentration:	0.1 μM
Incubation Time:	24 h
Result:	Effectively caused cell apoptosis, the percentage of apoptosis cells increased to 54%

Western Blot Analysis

Cell Line:	HepG2 cells^[1]
Concentration:	0.1 μM
Incubation Time:	24 h
Result:	Showed strongly effects on inducing the proteolytic cleavage of PARP and up-regulating the expression level of caspase-3, which could lead to cell death at last.

RT-PCR

Cell Line:	HepG2 cells^[1]
Concentration:	0.05 μM
Incubation Time:	24, 48 and 72 h
Result:	Markedly decreased mRNA expression level of TDO at a time-dependent manner.

In Vivo

IDO/Tubulin-IN-2 (HT2) (30 mg/kg; IV; daily, for 21 days) significantly inhibits tumor growth^[1].
IDO/Tubulin-IN-2 (30 mg/kg; IV; 29 days) has effective antitumor immunity ability to promote the tumor therapeutic efficacy^[1].

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

Animal Model:	ICR mice (mouse liver cancer xenograft models, established by subcutaneous inoculation of H22 cells)^[1]
Dosage:	30 mg/kg
Administration:	Intravenously injected via a tail vein; daily, for 21 days
Result:	Significantly inhibited tumor growth.

Animal Model:	Male A549 tumor xenograft BALB/c nude mice (5 weeks, 18-22 g)^[1]
Dosage:	30 mg/kg
Administration:	IV, daily, for 29 days
Result:	Had effective antitumor immunity ability to promote the tumor therapeutic efficacy.

Molecular Weight

860.87

Formula

C₄₈H₄₀N₆O₁₀

CAS No.

2409479-24-7

SMILES

COC1=CC=C(C=C1OC(C2=CC=CC(CN3C=C(N=N3)CCOC(C4=CC=CC(CN5N=NC6=C5C(C7=CC=CC=C7C6=O)=O)=C4)=O)=C2)=O)/C=C\C8=CC(OC)=C(C(OC)=C8)OC

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]. Hua S, Chen F, Gou S. Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase. Eur J Med Chem. 2020;187:111949. [Content Brief]

IDO/Tubulin-IN-2 Related Classifications

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
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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:

IDO/Tubulin-IN-22409479-24-7Microtubule/TubulinApoptosisAntitumorHepG2A549 cellsLow toxicityICR miceBALB/c nude miceInhibitorinhibitorinhibit

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