[CAS NO. 1616632-77-9] TIC10

Name: TIC10
Brand: Arctom Scientific
SKU: HY-15615A

Ships within

Stock

Price

Qty

Total

$0.00

Please click "REQUEST A QUOTE" button if you need other sizes or custom synthesis

request a quote

If there is no stock, or you need other sizes or custom synthesis, please:

PRODUCTS SPECIFICATIONS [1616632-77-9]

Distributor

Catalog

HY-15615A

Brand

MCE

CAS

1616632-77-9

DESCRIPTION [1616632-77-9]

Overview

MDL	MFCD28118993
Molecular Weight	386.49
Molecular Formula	C24H26N4O
SMILES	O=C1N(CC2=CC=CC=C2C)C3=NCCN3C4=C1CN(CC5=CC=CC=C5)CC4

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

5 Publications Citing Use of MCE

Summary

TIC10 (ONC-201) is a potent, orally active, and stable tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) inducer which acts by inhibiting Akt and ERK , consequently activating Foxo3a and significantly inducing cell surface TRAIL. TIC10 can cross the blood-brain barrier ^[1] .

IC50 & Target

TRAIL

In Vitro

TIC10 transcriptionally induces TRAIL in a p53-independent manner and crosses the blood-brain barrier ^[1] .
TIC10 induces a sustained up-regulation of TRAIL in tumors and normal cells that may contribute to the demonstrable antitumor activity of TIC10 ^[1] .
TIC10 inactivates kinases Akt and extracellular signal-regulated kinase (ERK), leading to the translocation of Foxo3a into the nucleus, where it binds to the TRAIL promoter to up-regulate gene transcription ^[1] .
TIC10 is an efficacious antitumor therapeutic agent that acts on tumor cells and their micro-environment to enhance the concentrations of the endogenous tumor suppressor TRAIL ^[1] .
TIC10 also causes a down-regulation of the total expression of ERK ^[1] .

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

In Vivo

In DLD-1 colon cancer xenografts, TIC10 induces tumor stasis at 1 week after treatment, whereas TRAIL-treated tumors progress after a single dose. A single dose of TIC10 also induces a sustained regression of the SW480 xenograft and is equally effective when delivered by intraperitoneal or oral route, suggesting favorable oral bioavailability for TIC10. Titration of a single oral dose of TIC10 in the HCT116 xenograft model reveals sustained antitumor efficacy at 25 mg/kg. Exposure to oral TIC10 at 25 mg/kg weekly for 4 weeks in immunocompetent mice does not cause any changes in selected serum chemistry markers. The same oral dosing schedule is applied to Eμ-myc transgenic mice, which spontaneously develop meta-static lymphoma from weeks 9 to 12 of age, and TIC10 significantly (P=0.00789) prolongs the survival of these mice by 4 weeks ^[1] .

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT03791398	Brown University\|Rhode Island Hospital\|Bristol-Myers Squibb\|Oncoceutics, Inc.	Metastatic Colorectal Cancer	November 15, 2019	Phase 1\|Phase 2
NCT05542407	UNC Lineberger Comprehensive Cancer Center\|Genentech, Inc.\|Oncoceutics, Inc.	Endometrial Cancer\|Metastasis	November 15, 2022	Phase 1
NCT05476939	Gustave Roussy, Cancer Campus, Grand Paris\|Chimerix\|Innovative Therapies For Children with Cancer Consortium	Diffuse Intrinsic Pontine Glioma\|Diffuse Midline Glioma, H3 K27M-Mutant	September 29, 2022	Phase 3
NCT05009992	University of California, San Francisco\|The Chad-Tough Defeat DIPG Foundation\|Mithil Prasad Foundation\|Storm the Heavens Fund\|National Institute of Neurological Disorders and Stroke (NINDS)	Diffuse Intrinsic Pontine Glioma\|Diffuse Midline Glioma, H3 K27M-Mutant\|Recurrent Diffuse Intrinsic Pontine Glioma\|Recurrent Diffuse Midline Glioma, H3 K27M-Mutant\|Recurrent WHO Grade III Glioma\|WHO Grade III Glioma	October 20, 2021	Phase 2
NCT03485729	Chimerix	Endometrial Cancer Recurrent	March 21, 2018	Phase 2
NCT05392374	Chimerix	Glioma
NCT03733119	University of Wisconsin, Madison\|The V Foundation for Cancer Research	Triple Negative Breast Cancer	November 13, 2018	Phase 2
NCT02420795	M.D. Anderson Cancer Center\|National Cancer Institute (NCI)	Central Nervous System Lymphoma\|Gastric Mantle Cell Lymphoma\|Recurrent Mantle Cell Lymphoma\|Recurrent Non-Hodgkin Lymphoma\|Refractory Mantle Cell Lymphoma\|Refractory Non-Hodgkin Lymphoma\|Splenic Mantle Cell Lymphoma	November 3, 2015	Phase 1\|Phase 2
NCT04617002	Chimerix	Glioma\|H3 K27M
NCT04629209	Chimerix	Glioblastoma	February 15, 2021	Phase 2
NCT03394027	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	Triple Negative Breast Cancer\|Endometrial Cancer\|Hormone Receptor Positive, HER2 Negative Breast Cancer	January 17, 2018	Phase 2
NCT03932643	Vijaya Bhatt\|University of Nebraska	Acute Myeloid Leukemia\|Myelodysplastic Syndromes	July 30, 2019	Phase 1
NCT02863991	Chimerix	Multiple Myeloma	January 1, 2016	Phase 1\|Phase 2
NCT03099499	Fox Chase Cancer Center\|Oncoceutics, Inc.	Endometrial Cancer	June 8, 2017	Phase 2
NCT03295396	Chimerix	Glioma	October 31, 2017	Phase 2
NCT02609230	Fox Chase Cancer Center	Advanced Solid Tumors\|Multiple Myeloma	November 5, 2015	Phase 1
NCT03416530	Chimerix	Diffuse Intrinsic Pontine Glioma\|Glioma, Malignant	January 29, 2018	Phase 1
NCT02525692	Chimerix	Glioblastoma\|Diffuse Midline Glioma\|H3 K27M Glioma\|Thalamic Glioma\|Infratentorial Glioma\|Basal Ganglia Glioma	January 2016	Phase 2
NCT02250781	Rutgers, The State University of New Jersey\|National Cancer Institute (NCI)\|Rutgers Cancer Institute of New Jersey	Solid Tumors	January 12, 2015	Phase 1
NCT03034200	Peter Anderson\|Case Comprehensive Cancer Center	Recurrent Neuroendocrine Tumor\|Metastatic Neuroendocrine Tumor	August 2, 2017	Phase 2
NCT04854044	Jonsson Comprehensive Cancer Center\|National Cancer Institute (NCI)\|Oncoceutics, Inc.\|University of California, Los Angeles	Recurrent Glioblastoma\|Recurrent Gliosarcoma\|Recurrent Supratentorial Glioblastoma\|Supratentorial Gliosarcoma	May 1, 2021	Phase 1
NCT02392572	M.D. Anderson Cancer Center\|Oncoceutics, Inc.	Recurrent Acute Lymphoblastic Leukemia\|Recurrent Acute Myeloid Leukemia\|Recurrent Myelodysplastic Syndrome\|Refractory Acute Lymphoblastic Leukemia\|Refractory Acute Myeloid Leukemia\|Refractory Myelodysplastic Syndrome	November 3, 2015	Phase 1\|Phase 2
NCT05580562	Chimerix	H3 K27M\|Glioma	November 15, 2022	Phase 3
NCT02324621	Rutgers, The State University of New Jersey\|National Cancer Institute (NCI)\|Rutgers Cancer Institute of New Jersey\|Oncoceutics, Inc.	Unspecified Adult Solid Tumor	February 20, 2015	Phase 1
NCT02038699	Chimerix	Advanced Glioblastoma\|Advanced Colorectal Cancer\|Advanced Triple-negative Breast Cancer\|Advanced Non-small Cell Lung Cancer	January 2014	Phase 1\|Phase 2
NCT03134131	Chimerix	Glioma
NCT03492138	Ajai Chari\|Icahn School of Medicine at Mount Sinai	Multiple Myeloma	March 26, 2018	Phase 1\|Phase 2
NCT04055649	Ira Winer\|Barbara Ann Karmanos Cancer Institute	Malignant Ovarian Epithelial Tumor\|Platinum-Resistant Fallopian Tube Carcinoma\|Platinum-Resistant Ovarian Carcinoma\|Platinum-Resistant Primary Peritoneal Carcinoma\|Recurrent Fallopian Tube Carcinoma\|Recurrent Ovarian Carcinoma\|Recurrent Primary Peritoneal Carcinoma\|Refractory Fallopian Tube Carcinoma\|Refractory Ovarian Carcinoma\|Refractory Primary Peritoneal Carcinoma	January 21, 2020	Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 9.38 mg/mL ( 24.27 mM ; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5874 mL	12.9369 mL	25.8739 mL
5 mM	0.5175 mL	2.5874 mL	5.1748 mL
10 mM	0.2587 mL	1.2937 mL	2.5874 mL

* Please refer to the solubility information to select the appropriate solvent.

References

[1] Allen JE, et al. Dual inactivation of Akt and ERK by TIC10 signals Foxo3a nuclear translocation, TRAIL gene induction, and potent antitumor effects. Sci Transl Med. 2013 Feb 6;5(171):171ra17.