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Rabusertib

Catalog No. T6084 CAS 911222-45-2

Synonyms: LY2603618, IC-83

Rabusertib (IC-83) is an inhibitor of the cell cycle checkpoint kinase 1 (chk1) 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.

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Rabusertib, CAS 911222-45-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 31.00
2 mg	In stock	$ 42.00
5 mg	In stock	$ 67.00
10 mg	In stock	$ 116.00
25 mg	In stock	$ 219.00
50 mg	In stock	$ 366.00
100 mg	In stock	$ 515.00
200 mg	In stock	$ 658.00
500 mg	In stock	$ 996.00
1 mL * 10 mM (in DMSO)	In stock	$ 77.00

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Purity: 99.63%

Purity: 99.40%

Purity: 98.86%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Rabusertib (IC-83) is an inhibitor of the cell cycle checkpoint kinase 1 (chk1) 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	Chk1:7 nM
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].

Synonyms	LY2603618, IC-83
Molecular Weight	436.3
Formula	C18H22BrN5O3
CAS No.	911222-45-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 11 mg/mL (25.2 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

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.

Citations

1. Zhang L, Wirth M, Patra U, et al.Actionable loss of SLF2 drives B‐cell lymphomagenesis and impairs the DNA damage response.EMBO Molecular Medicine.2023: e16431.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Inhibitor Library Anti-Cancer Active Compound Library Highly Selective Inhibitor Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Anti-Cancer Drug Library NO PAINS Compound Library Bioactive Compounds Library Max Anti-Liver Cancer Compound Library

Related Products

Related compounds with same targets

CCT241533 hydrochloride GDC0575 monohydrochloride SB-218078 CCT241533 M443 Tuvusertib GDC-0575 BX-912

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Rabusertib 911222-45-2 Autophagy Cell Cycle/Checkpoint PI3K/Akt/mTOR signaling PDK Chk inhibit LY2603618 Inhibitor IC-83 IC 83 Checkpoint Kinase (Chk) LY 2603618 IC83 LY-2603618 inhibitor

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