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35943-35-2 (Triciribine)

1

Identification

Triciribine Triciribine
Name Triciribine
Formula C13H16N6O4
MW 320.3
CAS No. 35943-35-2
EINECS
Smiles NC1=NN(C)C2=NC=NC3=C2C1=CN3[[email protected]@H]([[email protected]](O)[[email protected]@H]4O)O[[email protected]@H]4CO
Synonyms 1,5-Dihydro-5-methyl-1-beta-D-ribofuranosyl-1,4,5,6,8-pentaazaacenaphthylen-3-amine; (2R,3R,4S,5R)-2-(3-amino-5-methyl-1,4,5,6,8-pentaazaacenaphthylen-1(5H)-yl)-5-(hydroxymethyl)tetrahydrofuran-3,4-diol
InChI InChI=1S/C13H16N6O4/c1-18-11-7-5(10(14)17-18)2-19(12(7)16-4-15-11)13-9(22)8(21)6(3-20)23-13/h2,4,6,8-9,13,20-22H,3H2,1H3,(H2,14,17)/t6-,8-,9-,13-/m1/s1
2

Introduction

Triciribine(API-2; NSC 154020) is a DNA synthesis inhibitor, also inhibits Akt and HIV-1 with IC50 of 130 nM and 20 nM, respectively; does not inhibit PI3K/PDK1; 5000-fold less active in cells lacking adenosine kinase. IC50 value: 130 nM (Akt); 20 nM (HIV1) Triciribine, also known as API-2, suppresses the phosphorylation level and kinase activity of Akt.

Background Information

Triciribine, also known as API-2, NSC 154020, is a cell-permeable tricyclic nucleoside that inhibits the phosphorylation, activation, and signalling of Akt-1, -2, and -3. Akt-1, -2, and -3 are serine/threonine protein kinases in the phosphatidylinositol 3 (PI3)-kinase signalling pathway that play a critical role in the regulation of cell proliferation and survival. Triciribine induced autophagy, which could be interpreted as a defensive mechanism, because an autophagy inhibitor (chloroquine) increased triciribine-induced apoptosis. In vitro, Triciribine (API-2) significantly inhibits Akt-overexpressing human cancer cell lines growth with 50% inhibition at ~5-10 µM. It also inhibits DNA synthesis and displays antiviral activity against HIV-1 and -2. Combinations of triciribine with classic inhibitors targeting other molecules of the PI3K-AKT-pathway led to synergistic anti-proliferative effects. ......by AbMole BioScience
Triciribine, also known as API-2, suppresses the phosphorylation level and kinase activity of Akt. ......by AdooQ BioScience, LLC
Description ......by Apexbio Technology LLC
Triciribine is a potent AKT inhibitor and a cell-permeable tricyclic nucleoside molecule with potential antineoplastic activity. Akt-1, -2, and -3 are serine/threonine protein kinases in the phosphatidylinositol (PI3)-kinase signalling pathway that play a ......by BOC Sciences
Cell-permeable. A synthetic tricyclic nucleoside which acts as a specific inhibitor of the Akt signaling pathway. It selectively inhibits the phosphorylation and activation of Akt1, -2 and -3 but does not inhibit Akt kinase activity nor known upstream Akt activators such as PI 3-Kinase and PDK1. ......by BioVision, Inc.,
Triciribine is a DNA synthesis inhibitor, also inhibits Akt and HIV-1/2 with IC50 of 130 nM, and 0.02-0.46 μM, respectively. ......by MedChemexpress Co., Ltd.
Triciribine, also known as VQD-002, is a potent AKT inhibitor and a cell-permeable tricyclic nucleoside molecule with potential antineoplastic activity. Triciribine inhibits the phosphorylation, activation, and signalling of Akt-1, -2, and -3, which may result in the inhibition of Akt-expressing tumor cell proliferation. Akts are anti-apoptotic serine/theronine-specific protein kinases that phosphorylate and inactivate components of the apoptotic machinery, including Bcl-xL/Bcl-2-associated death promoter (BAD) and caspase 9. ......by MedKoo Biosciences, Inc.
Triciribine is a DNA synthesis inhibitor, also inhibits Akt in PC3 cell line and HIV-1 in CEM-SS, H9, H9IIIB, U1 cells with IC50 of 130 nM and 20 nM, respectively; does not inhibit PI3K/PDK1; 5000-fold less active in cells lacking adenosine kinase. Phase 1/2. ......by Selleck Chemicals LLC
Triciribine is a DNA synthesis inhibitor, also inhibits Akt and HIV-1 with IC50 of 130 nM and 20 nM, respectively; does not inhibit PI3K/PDK1; 5000-fold less active in cells lacking adenosine kinase. Phase 1/2. ......by Target Molecule Corp.
Selective inhibitor of Akt (protein kinase B) signaling; displays minimal inhibition of PKC, PKA, SGK and p38 pathways. Inhibits phosphorylation and activation of downstream targets of Akt including Bad, GSK-3β and AFX. Induces apoptosis and growth arrest in vitro, preferentially in human cancer cells with elevated levels of Akt. Potently and selectively inhibits growth of Akt-overexpressing tumors in mice. Inhibits DNA synthesis and displays antiviral activity against HIV-1 and -2. ......by Tocris Bioscience Inc.
3

Protocol(Only for Reference)

Cell Experiment

Animal Experiment

Animal Models OVCAR3, OVCAR8, PANC1, OVCAR5 and COLO357 tumor cells are injected s.c. into 80week-old female nude mice.
Dosage 1 mg/kg/day
Formulation Triciribine is dissolved in 20% DMSO.
Administration Triciribine is administrated through i.p. injection once a day.
Source Selleck Chemicals LLC
4

Physical and Chemical Properties

Appearance:Light yellow to yellow Solid EBNumber:EB000017954

Storage condition

Storage condition:Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). Stock solution storage:0 - 4 C for short term (days to weeks), or -20 C for long term (months). Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. by MedKoo Biosciences, Inc.

Solubility

DMSO > 50 mg/mL 1eq. HCl by MedChemexpress Co., Ltd.
Soluble in DMSO, not in water by MedKoo Biosciences, Inc.
(25°C) * In vitro DMSO 64 mg/mL (199.81 mM); Water<1 mg/mL (<1 mM); Ethanol<1 mg/mL (<1 mM); In vivo 1% DMSO+30% polyethylene glycol+1% Tween 8030 mg/mL by Selleck Chemicals LLC
5

Mechanism and Indication

6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
Triciribine Yeshiva University Metastatic breast cancer 2012/1/31 2014/6/30 Phase 2 Clinical
Triciribine H Lee Moffitt Cancer Center and Research Institute Ovary tumor 2013/12/31 2015/10/31 Phase 2 Clinical
Triciribine H Lee Moffitt Cancer Center and Research Institute Cancer 2006/4/30 2010/9/30 Phase 2 Clinical
Triciribine MD Anderson Cancer Center Leukemia 2006/8/31 2012/10/31 Phase 1 Clinical
Triciribine - Phase 2
7

Safety Data of Triciribine

8

Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
AbMole BioScience 10mg/USD150(In stock) USA
Abcam 1mg/USD135() USA
AdooQ BioScience, LLC USA
Apexbio Technology LLC 1mg/USD70(In stock) USA
Ark Pharm, Inc. USA
BOC Sciences
BioVision, Inc., 1mg/USD145() USA
Biochempartner Co., Ltd China
CHEMSCENE, LLC 5mg/USD96();10mg/USD156() USA
Cayman Chemical Company 1mg/USD117() USA
EMD Millipore 10mg/USD389() USA
MedChemexpress Co., Ltd. 5mg/USD96();10mg/USD156() USA
MedKoo Biosciences, Inc. USA
Selleck Bio USA
Selleck Chemicals LLC 5mg/USD120(In stock);10mM/1mLIn DMSO/USD150(In stock);10mg/USD170(In stock);10mM(in 1mL DMSO)/USD189(in 1mL DMSO);50mg/USD570(In stock);200mg/USD1670(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. 5mg/USD96();10mg/USD156() China
Target Molecule Corp. 2mg/USD51();5mg/USD87();10mg/USD115();25mg/USD198();50mg/USD358() USA
Tocris Bioscience Inc. 10mg/USD275() USA
Wuhan Vanzpharm Inc. China
10

Related Products

Other Forms of 35943-35-2

Name CAS No Formula MW
Triciribine phosphate 61966-08-3 C13H17N6O7P 400.28

Recommended Compounds in Nucleoside Antimetabolite/Analog Akt DNA/RNA Synthesis HIV

Name CAS No Formula MW
5-BrdU 59-14-3 C9H11BrN2O5 307.1
Vidarabine 5536-17-4 C10H13N5O4 267.24
Adenosine 58-61-7 C10H13N5O4 267.24
Carmofur 61422-45-5 C11H16FN3O3 257.26
Cytidine 65-46-3 C9H13N3O5 243.22
Merimepodib 198821-22-6 C23H24N4O6 452.46
Floxuridine 50-91-9 C9H11FN2O5 246.19
Dacarbazine 4342-03-4 C6H10N6O 182.18
Tipiracil (hydrochloride) 183204-72-0 C9H12Cl2N4O2 279.12
Trifluorothymidine 70-00-8 C10H11F3N2O5 296.2
Orotic acid 65-86-1 C5H4N2O4 156.1
Nelarabine 121032-29-9 C11H15N5O5 297.27
6-Mercaptopurine 50-44-2 C5H4N4S 152.18
LY2334737 892128-60-8 C17H25F2N3O5 389.39
Cytarabine (hydrochloride) 69-74-9 C9H14ClN3O5 279.68
Cytarabine 147-94-4 C9H13N3O5 243.22
Gemcitabine (elaidate) 210829-30-4 C27H43F2N3O5 527.6442
Tegafur 17902-23-7 C8H9FN2O3 200.17
Fludarabine 21679-14-1 C10H12FN5O4 285.23
TAS-102 733030-01-8 C20H28Cl2F3N7O6 590.38

Recommended Compounds in Same Indication

Name CAS No Formula MW
Volasertib 755038-65-4 C34H50N8O3 618.81
Olaparib 763113-22-0 C24H23FN4O3 434.46
PU-H71 873436-91-0 C18H21IN6O2S 512.37
Ostarine 841205-47-8 C19H14F3N3O3 389.33
IDO5L 914471-09-3 C9H7ClFN5O2 271.6356
MK-0752 471905-41-6 C21H21ClF2O4S 442.9
Tivozanib 475108-18-0 C22H19ClN4O5 454.86
Cyclophosphamide 50-18-0 C7H15Cl2N2O2P 261.09
Fenretinide 65646-68-6 C26H33NO2 391.55
Retaspimycin 857402-23-4 C31H45N3O8 587.7
Retaspimycin (Hydrochloride) 857402-63-2 C31H46ClN3O8 624.17
LY2228820 862507-23-1 C26H37FN6O6S2 612.74
Octreotide (acetate) 79517-01-4 C51H70N10O12S2 1079.29
Litronesib 910634-41-2 C23H37N5O4S2 511.701
LY2603618 911222-45-2 C18H22BrN5O3 436.3
Ganetespib 888216-25-9 C20H20N4O3 364.4
Ixabepilone 219989-84-1 C27H42N2O5S 506.7
Palifosfamide 31645-39-3 C4H11Cl2N2O2P 221.02
Carboplatin 41575-94-4 C6H12N2O4Pt 371.25
Foretinib 849217-64-7 C34H34F2N4O6 632.65
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Route of Synthesis

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References

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More Information

Triciribine

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