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PI3K/Akt/mTOR signaling PDK Rabusertib

Rabusertib

Catalog No. T6084   CAS 911222-45-2
Synonyms: IC-83, LY2603618, LY2603618 IC-83

Rabusertib is an inhibitor of the cell cycle checkpoint kinase 2 (chk2) with potential chemopotentiating activity. Rabusertib has been used in trials studying the treatment of Cancer, Solid Tumors, Advanced Cancer, Pancreatic Neoplasms, and Non-Small Cell Lung Cancer.

Rabusertib, CAS 911222-45-2
Pack Size Availability Price/USD Quantity
2 mg In stock 55.00
5 mg In stock 93.00
10 mg In stock 139.00
25 mg In stock 232.00
50 mg In stock 417.00
100 mg In stock 751.00
1 mL * 10 mM (in DMSO) In stock 98.00
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Biological Description
Chemical Properties
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Description Rabusertib is an inhibitor of the cell cycle checkpoint kinase 2 (chk2) with potential chemopotentiating activity. Rabusertib has been used in trials studying the treatment of Cancer, Solid Tumors, Advanced Cancer, Pancreatic Neoplasms, and Non-Small Cell Lung Cancer.
Targets&IC50 Chk1 : ic50 7nM,   PDK1 : ic50 893nM,  
In vitro Chk1 is an ATP-dependent serine-threonine kinase and a key component in the DNA replication-monitoring checkpoint system activated by double-stranded breaks (DSBs). Chk1 contributes to all currently defined cell cycle checkpoints, including G1/S, intra-S-phase, G2/M, and the mitotic spindle checkpoint. By inhibiting the activity of chk1, LY2603618 prevents the repair of DNA caused by DNA-damaging agents, thus potentiating the antitumor efficacies of various chemotherapeutic agents. However, preClinicalal data involving LY2603618 has not been published until now. [1] Inhibition of Chk1 is predicted to enhance the effects of antimetabolites, such as gemcitabine. [2] LY2603618 treatment impairs DNA synthesis, increases DNA damage (via mitotic defects), induces apoptosis, and has synergistic activity with pemetrexed, especially in p53 mutant tumor cells. [3]
In vivo In xenograft models, LY2603618 delays tumor growth when given in combination with pemetrexed. [3]
Kinase Assay Protein kinase assays are performed variously. Assays are performed on the following protein kinases: ABL, AKT1, ARG, CAMK2, CDK1, CDK2, CHK1, CHK2, DAPK1, EGFR, EPHA1, EPHB2, EPHB3, EPHB4, ERK1, ERK2, FES, FGFR1, FGFR3, FGFR4, FGR, HCK, HER2, INSR, JNK1, JNK2, LCK, MET, NTRK1, NTRK2, p38α, p38β, p38δ, p38γ, p70S6K, PDGFRα, PDGFRβ,, PDK1, PKCα, ROCK2, ROS, RSK2, SGK1, SRC, SYK, TAK1, TYRO3, VEGFR2, VEGFR3, YES, ZAP70[1].
Cell Research
LY2603618 is prepared in DMSO (10 mM) and stock, and then diluted 1000-fold into medium[1]. Cells are plated at 2.5×103 per well, on 96-well tissue culture plates and incubated for one cell doubling (18-24 h). Gemcitabine dilutions are set up by half-log steps across a final concentration range of 1-1000 nM. LY2603618 is prepared by dilutions in DMSO to 5000× final concentration, and then diluted 1000-fold into medium to generate 5× stocks for addition to wells. Approximately 24 h after Gemcitabine addition, LY2603618 is added. Each combination is done in triplicate. After a period of two cell doublings following LY2603618 addition, MTS/PMS reagent is added to each well according to the manufacturer’s instructions. Absorbance is read on a Spectra Max 250 spectrophotometer at 490 nm and the data analyzed with GraphPad Prism 4.0. Dose-response curves are fit by non-linear regression, with bottom fits constrained to 0 % inhibition[1].
Animal Research
Animal Model: Harlan athymic nude mice
Synonyms IC-83 , LY2603618 , LY2603618 IC-83
Purity 99.63%
Molecular Weight 436.3
Formula C18H22BrN5O3
CAS No. 911222-45-2

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 11 mg/mL (25.2 mM)

Ethanol: <1 mg/mL

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Solution 1

2% DMSO/30% PEG400/0.5% Tween80/5% Propylene glycol: 30mg/mL

Citations

References and Literature
1. King C, et al. Invest New Drugs. 2014, 32(2):213-26. 2. Emiliano Calvo1, et al. Mol Cancer Ther, 2011, A94. 3. Govindan R. J Thorac Oncol, 2011, 6(11 Suppl 4), S1757.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Clinical Compound Library Autophagy Compound Library PI3K-AKT-mTOR Compound Library DNA Damage & Repair Compound Library Kinase Inhibitor Library Anti-cancer Clinical Compound Library Anti-cancer Metabolism Compound Library Cell cycle related Compound Library

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