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Prexasertib

Cat. No. M13622

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Prexasertib Structure
Synonym:

LY2606368

Size Price Availability Quantity
1mg USD 50 In stock
5mg USD 127 In stock
25mg USD 395 In stock
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Quality Control & Documentation
Biological Activity

Prexasertib (LY2606368) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib shows potent anti-tumor activity.

Chemical Information
Molecular Weight 365.39
Formula C18H19N7O2
CAS Number 1234015-52-1
Form Solid
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Jason Ostergaard, et al. Br J Haematol. Preclinical efficacy of prexasertib in acute lymphoblastic leukemia

[2] Chenguang Liu, et al. Nat Chem. Automated synthesis of prexasertib and derivatives enabled by continuous-flow solid-phase synthesis

[3] Giulio Evangelisti, et al. Expert Opin Investig Drugs. Prexasertib: an investigational checkpoint kinase inhibitor for the treatment of high-grade serous ovarian cancer

[4] Yoshihito Morimoto, et al. Oncol Rep. Prexasertib increases the sensitivity of pancreatic cancer cells to gemcitabine and S‑1

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AZD7762 is a potent ATP-competitive checkpoint kinase inhibitor with an IC50 of 5 and <10 nM for CHK1 and CHK2 respectively.

BIBR1532

BIBR1532 is a potent and selective telomerase inhibitor with IC50 of 100 nM. BIBR 1532 inhibits the proliferation of JVM13 leukemia cells with an IC50 of 52 μM, and similar effect also occurs in other leukemia cell lines such as Nalm-1, HL-60, and Jurkat. BIBR1532 is also an inhibitor of TERT, the rate-limiting enzyme in the regulation of telomerase activity.

PF-477736

PF-477736 is a selective checkpoint kinase 1 (Chk1) inhibitor with Ki values of 0.49 nM and 47 nM for CHK1 and CHK2 respectively.

SCH 900776

SCH 900776 (MK-8776) is a highly potent and functionally selective CHK1 inhibitor with IC50 of 3 nM.

Rabusertib (LY2603618)

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

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Abmole Inhibitor Catalog




Keywords: Prexasertib, LY2606368 supplier, Checkpoint, inhibitors, activators

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