1. Cell Cycle/DNA Damage
    Autophagy
  2. Checkpoint Kinase (Chk)
    Autophagy
  3. Rabusertib

Rabusertib (Synonyms: LY2603618; IC-83)

Cat. No.: HY-14720 Purity: 99.69%
Handling Instructions

Rabusertib (LY2603618) is a potent and selective inhibitor of Chk1 with an IC50 of 7 nM.

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

Rabusertib Chemical Structure

Rabusertib Chemical Structure

CAS No. : 911222-45-2

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10 mM * 1 mL in DMSO USD 119 In-stock
Estimated Time of Arrival: December 31
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10 mg USD 168 In-stock
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100 mg USD 840 In-stock
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Based on 3 publication(s) in Google Scholar

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Description

Rabusertib (LY2603618) is a potent and selective inhibitor of Chk1 with an IC50 of 7 nM.

IC50 & Target[1]

Chk1

7 nM (IC50)

Chk2

12000 nM (IC50)

PDK1

893 nM (IC50)

CAMK2

1550 nM (IC50)

VEGFR3

2128 nM (IC50)

MET

2200 nM (IC50)

JNK1

4930 nM (IC50)

RSK2

5700 nM (IC50)

NTRK1

12000 nM (IC50)

In Vitro

Rabusertib (LY2603618) is a highly effective inhibitor of multiple aspects of Chk1 biology. Rabusertib (LY2603618) is tested against a panel of 51 diverse protein kinases in vitro. With an IC50 of 7 nM for Chk1, Rabusertib (LY2603618) is approximately 100-fold more potent against Chk1 than against any of the other protein kinases evaluated (PDK1, IC50=893 nM, others >1000 nM). Rabusertib (LY2603618) effectively reduced Chk1 autophosphorylation with an EC50 of 430 nM. Inhibition of Chk1 by Rabusertib (LY2603618) also effectively abrogated the G2/M DNA damage checkpoint in cells treated with DNA damaging agents. Treatment of cells with Rabusertib (LY2603618) produced a cellular phenotype similar to that reported for depletion of Chk1 by RNAi. Inhibition of intracellular Chk1 by Rabusertib (LY2603618) results in impaired DNA synthesis, elevated H2A.X phosphorylation indicative of DNA damage and premature entry into mitosis[1]. Treatments of the SK-N-BE(2) cells with variable concentrations of Rabusertib (LY2603618) results in dose-dependent inhibition of cell growth determined by MTT assays with an IC50 of 10.81 µM[1].

In Vivo

Mice bearing Calu-6 xenografts are treated with 150 mg/kg (IP) Gemcitabine and a single simultaneous 200 mg/kg oral dose of Rabusertib (LY2603618). 200 mg/kg of Rabusertib (LY2603618) is sufficient to inhibit 85 % of Chk1 autophosphorylation in vivo at 2 h. Rabusertib (LY2603618) effectively reduces Gemcitabine-induced phosphorylation on Tlk serine 695 as well, supporting the cited report with a selective chemical inhibitor of Chk1[1].

Clinical Trial
Molecular Weight

436.30

Formula

C₁₈H₂₂BrN₅O₃

CAS No.

911222-45-2

SMILES

BrC(C=C1NC(NC2=NC=C(N=C2)C)=O)=C(C=C1OC[[email protected]]3OCCNC3)C

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 : 50 mg/mL (114.60 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2920 mL 11.4600 mL 22.9200 mL
5 mM 0.4584 mL 2.2920 mL 4.5840 mL
10 mM 0.2292 mL 1.1460 mL 2.2920 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.73 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.73 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.73 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[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. Rabusertib (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, Rabusertib (LY2603618) is added. Each combination is done in triplicate. After a period of two cell doublings following Rabusertib (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].

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

Animal Administration
[1]

Mice[1]
Female Harlan athymic nude mice (26-28 g) are used for these studies. Tumor growth is initiated by subcutaneous injection of 1×106 Calu-6 cells in a 1:1 mixture of serum-free growth medium and Matrigel in the rear flank of each subject animal. When tumor volumes reach approximately 150 mm3 in size, the animals are randomized by tumor size and body weight, and placed into their respective treatment groups. Each animal receives 2 injections, one of either saline vehicle or 150 mg/kg Gemcitabine administered by intraperitoneal injection in a volume of 200 μL, and the other being the Captisol vehicle or LY2603618 administered orally in a volume of 200 μL.

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

References

Purity: 99.69%

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Rabusertib
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