Structure
(4-Hydroxyphenylbutazone, CAS 16860-43-8)
Prexasertib dimesylate Biochemical
Prexasertib dimesylate
Purity
98%
Synonyms
Prexasertib dimesylate; N/A; Prexasertib dimesylate biochemical
Purity/Purification
98%
CAS
1234015-58-7
Targets&IC50
Chk1:<1 nM (IC50), Chk1:0.9 nM (Ki), Chk2:8 nM (IC50)
Solubility
<1mg/ml refers to the product slightly soluble or insoluble
In vitro
Prexasertib dimesylate (LY2606368 dimesylate; 1-10 mg/kg; SC; twice daily for 3 days, rest 4 days; for three cycles) causes growth inhibition in tumor xenografts[1]. Prexasertib dimesylate (15 mg/kg; SC) causes CHK1 inhibition in the blood and the phosphorylation of both H2AX (S139) and RPA2 (S4/S8)[1]. Animal Model: Female CD-1 nu-/nu- mice (26-28 g) with Calu-6 cells[1]. Dosage: 1, 3.3, or 10 mg/kg. Administration: SC; twice daily for 3 days, rest 4 days; for three cycles. Result: Caused statistically significant tumor growth inhibition (up to 72.3%). Animal Model: Female CD-1 nu-/nu- mice (26-28 g) with Calu-6 cells[1]. Dosage: 15 mg/kg (Pharmacokinetic Analysis). Administration: SC (200 uL). Result: CHK1 was 7 ng/mL at 12 hours and 3 ng/mL by 24 hours in plasma exposures. Phosphorylation of both H2AX (S139) and RPA2 (S4/S8) was detectable at 4 hours, showing the rapid occurrence of DNA damage.
Preparation and Storage
Powder: -20 degree C for 3 years
In solvent: -80 degree C for 2 years
In solvent: -80 degree C for 2 years
Structure
(4-Hydroxyphenylbutazone, CAS 16860-43-8)
Structure
(4-Hydroxyphenylbutazone, CAS 16860-43-8)
Structure
(4-Hydroxyphenylbutazone, CAS 16860-43-8)
Structure
(4-Hydroxyphenylbutazone, CAS 16860-43-8)
Related Product Information for Prexasertib dimesylate biochemical
Prexasertib dimesylate (LY2606368 dimesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a K i of 0.9 nM and an IC 50 of <1 nM. Prexasertib dimesylate inhibits CHK2 (IC 50 =8 nM) and RSK1 (IC 50 =9 nM). Prexasertib dimesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dimesylate shows potent anti-tumor activity.
References
1. Hughes MF, et, al. Prostaglandin hydroperoxidase-dependent oxidation of phenylbutazone: relationship to inhibition of prostaglandin cyclooxygenase. Mol Pharmacol. 1988 Aug;34(2):186-93.
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Product Notes
The Prexasertib dimesylate (Catalog #AAA227531) is a Biochemical and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "Prexasertib dimesylate, Biochemical" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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