Cat. No.: HY-111175

IG-105

Name: IG-105
Brand: MedChemExpress
SKU: HY-111175
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IG-105 is an orally active and potent tubulin inhibitor that competitively inhibits [³H] colchicine binding to tubulin with an IC₅₀ of 0.6 μM and inhibits tubulin polymerization with an IC₅₀ of 3 μM. IG-105 inhibits microtubule polymerization by binding to the colchicine pocket of tubulin, induces G2-M phase arrest, and subsequently activates the caspase cascade through Bcl-2 inactivation and p53 upregulation, inducing apoptosis. IG-105 effectively overcomes multidrug resistance as a non-Pgp substrate. IG-105 can be used for research on leukemia, breast cancer, liver cancer, prostate cancer, lung cancer, melanoma, pancreatic cancer, and colon cancer.

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CAS No.: 905978-63-4
Formule: C₂₀H₁₉N₃O₄S
Masse moléculaire:397.45

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Please store the product under the recommended conditions in the Certificate of Analysis.

IG-105 Chemical Structure

CAS No.: 905978-63-4

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Activité biologique
- Description
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

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Cellular Effect

Cell Line	Type	Value	Description	References
LoVo	IC₅₀	0.298 μM	Antiproliferative activity against human LoVo colon cancer cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay. Antiproliferative activity against human LoVo colon cancer cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.	18829501
NCI-H23	IC₅₀	0.274 μM	Antiproliferative activity against human NCI-H23 lung cancer cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay. Antiproliferative activity against human NCI-H23 lung cancer cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.	18829501
HUVEC	IC₅₀	2.52 μM	Antiproliferative activity against non-malignant human HUVEC cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay. Antiproliferative activity against non-malignant human HUVEC cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.	18829501
SMMC-7721	IC₅₀	0.528 μM	Antiproliferative activity against drug-resistant human SMMC-7721 hepatoma cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay. Antiproliferative activity against drug-resistant human SMMC-7721 hepatoma cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.	18829501
Bel-7402	IC₅₀	0.179 μM	Antiproliferative activity against naive human Bel-7402 hepatoma cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay. Antiproliferative activity against naive human Bel-7402 hepatoma cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.	18829501
MCF7-DOX	IC₅₀	0.199 μM	Antiproliferative activity against Pgp-overexpressing drug-resistant human MCF-7/Dox/Pgp breast cancer cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay. Antiproliferative activity against Pgp-overexpressing drug-resistant human MCF-7/Dox/Pgp breast cancer cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.	18829501
MCF7	IC₅₀	0.151 μM	Antiproliferative activity against naive human MCF-7 breast cancer cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay. Antiproliferative activity against naive human MCF-7 breast cancer cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.	18829501

In Vitro

IG-105 (up to 1 μM; 72 h) exerts significant inhibitory effects on cell growth and viability in CEM, Molt-3, DND-1, MIA PaCa-2, MCF-7, Bel-7402, SW620, LoVo, DU-145, NCI-H23, SMMC-7721, MCF-7/Dox/Pgp and HUVEC cells, with IC₅₀ values ranging from 0.012 to 0.298 μM; in contrast, its inhibitory activity against non-malignant HUVEC cells is much weaker (IC₅₀ = 2.52 μM)^[1].
IG-105 (2 μM) does not stimulate P-glycoprotein (Pgp) ATPase activity in a cell-free system^[1].
IG-105 (0.16-6 μM; 30 min) potently inhibits tubulin polymerization in a cell-free system with an IC₅₀ of 3 μM. It also competitively inhibits [³H]colchicine binding with an IC₅₀ of 0.6 μM, and does not interact with the vinca alkaloid binding pocket^[1].
IG-105 (0.35 μM; 12 h) disrupts the cellular microtubule network and induces microtubule depolymerization in human hepatocellular carcinoma Bel-7402 cells^[1].
IG-105 (0.35 μM; 3-36 h) induces G₂-M phase arrest in human hepatocellular carcinoma cell line Bel-7402, upregulates cyclin B1 protein expression and downregulates cyclin D1 protein expression in a time-dependent manner, induces Bcl-2 phosphorylation, promotes caspase-3 cleavage, and upregulates the expressions of p53 and p21^[1].
IG-105 (0.086-0.346 μM for 48 h and 0.35 μM for 12-48 h) induces apoptotic DNA fragmentation in human hepatocellular carcinoma Bel-7402 cells^[1].
IG-105 (0.35 μM; 6-24 h) significantly enhances the activities of caspase-9, caspase-8, and caspase-3 in human hepatocellular carcinoma Bel-7402 cells^[1].

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

Cell Cycle Analysis^[1]

Cell Line:

Bel-7402
Concentration:

0.35 μM
Incubation Time:

3, 6, 9, 12, 18, 24 h
Result:

Induced a significant accumulation and arrest of cells in the G2-M phase, accompanied by a decrease in the number of cells in the G0-G1 phase.

Western Blot Analysis^[1]

Cell Line:

Bel-7402
Concentration:

0.35 μM
Incubation Time:

3, 6, 9, 12, 18, 24, 36 h
Result:

Led to a time-dependent up-regulation of mitotic cyclin B1 protein expression and a decrease in G0-G1 phase cyclin D1 protein expression.
Induced phosphorylation of Bcl-2 protein and cleavage activation of caspase-3, and caused time-dependent up-regulation of p53 and p21 protein expression.

Immunofluorescence^[1]

Cell Line:

Bel-7402
Concentration:

0.35 μM
Incubation Time:

12 h
Result:

Caused the disruption of the intracellular microtubule network, showing short and curled microtubule fragments, and resulted in reduced microtubule density.

Parmacokinetics

Species	Dose	Route	C_max	T_max	AUC_0-24	AUC_0-∞	T_1/2	MRT	CL/F	V_z/F
Rat^[2]	100 mg/kg	p.o.	162.4 ng/mL	0.5 h	762.9 ng·h/mL	767.3 ng·h/mL	3.3 h	4.3 h	134.3 L/h/kg	654.7 L/kg
Rat^[2]	250 mg/kg	p.o.	241.8 ng/mL	0.8 h	853.9 ng·h/mL	865.6 ng·h/mL	4.6 h	4.3 h	312.6 L/h/kg	2072.0 L/kg
Rat^[2]	1000 mg/kg	p.o.	270.8 ng/mL	0.6 h	922.7 ng·h/mL	945.4 ng·h/mL	5.2 h	4.9 h	1064.1 L/h/kg	7981.1 L/kg

In Vivo

IG-105 (100-275 mg/kg; i.p.; once every two days; starting on day 11 post tumor implantation) significantly and completely inhibits tumor growth in a subcutaneous xenograft model of human hepatocellular carcinoma^[1].
IG-105 (100-200 mg/kg; i.p.; once every two days; starting on day 14 after tumor inoculation) significantly inhibits tumor growth in a subcutaneous xenograft model of human breast cancer^[1].
IG-105 (175 mg/kg; i.p.; once every two days; starting on day 11 post tumor implantation) converts subcurative doses of drugs into a synergistic complete control of tumor growth when combined with Oxaliplatin (HY-17371) or Doxorubicin (HY-15142) in a human hepatocellular carcinoma subcutaneous xenograft model^[1].
IG-105 (400-1000 mg/kg; i.p.; single administration; observation for 15 days) exhibits favorable safety in the acute toxicity model of healthy mice, with no lethal or significant pathological toxicity observed^[1].

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

Animal Model:

Kunming mice (female, 18-20 g)^[1]
Dosage:

400 mg/kg; 550 mg/kg; 700 mg/kg; 850 mg/kg; 1000 mg/kg
Administration:

i.p.; single dose; for 15 days
Result:

Caused no death or body weight loss even at the extremely high dose of 1000 mg/kg.
Histopathologic examination (H&E staining) revealed no evidence of pathologic damage in major organs such as liver, kidney, heart, lung, and spleen.

Chemical Information

CAS No. 905978-63-4
Masse moléculaire 397.45
Formule C₂₀H₁₉N₃O₄S
SMILES

O=S(C1=CC2=C(C=C1)N(C)C3=C2C=CC=C3)(NC4=CC=C(OC)N=C4OC)=O
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Wang YM, et al. N-(2,6-dimethoxypyridine-3-yl)-9-methylcarbazole-3-sulfonamide as a novel tubulin ligand against human cancer. Clinical cancer research : an official journal of the American Association for Cancer Research. 2008 Oct 01;14(19):6218-27. [Content Brief]

[2]. Pang J, et al. Simplified LC-MS/MS method for quantification of IG-105, a novel tubulin ligand, and its application to the pharmacokinetic study in rats at the anticancer effective dose. Pharmazie. 2019 Feb 1;74(2):79-82.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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IG-105

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