1234015-57-6
1234015-57-6 structure
- Name: Prexasertib Mesylate Hydrate
- Chemical Name: Prexasertib Mesylate Hydrate
- CAS Number: 1234015-57-6
- Molecular Formula: C19H25N7O6S
- Molecular Weight: 479.51
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2019-02-08 20:58:42
- Modify Date: 2024-01-12 10:55:27
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Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is a potent, selective, ATP competitive CHK1 and CHK2 inhibitor, with a Ki of 0.9 nM for CHK1 and IC50s of <1 nM, 8 nM for CHK1 and CHK2, respectively. Prexasertib Mesylate Hydrate inhibits HT-29 CHK1 autophosphorylation (S296) and HT-29 CHK2 autophosphorylation (S516). Prexasertib Mesylate Hydrate shows potent anti-tumor activity, significantly abrogates the G2/M checkpoint in p53 deficient HeLa cells with an EC50 of 9 nM[1].
| Name | Prexasertib Mesylate Hydrate |
|---|---|
| Synonyms | Prexasertib (Mesylate Hydrate) |
| Description | Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is a potent, selective, ATP competitive CHK1 and CHK2 inhibitor, with a Ki of 0.9 nM for CHK1 and IC50s of <1 nM, 8 nM for CHK1 and CHK2, respectively. Prexasertib Mesylate Hydrate inhibits HT-29 CHK1 autophosphorylation (S296) and HT-29 CHK2 autophosphorylation (S516). Prexasertib Mesylate Hydrate shows potent anti-tumor activity, significantly abrogates the G2/M checkpoint in p53 deficient HeLa cells with an EC50 of 9 nM[1]. |
|---|---|
| Related Catalog | |
| Target |
Chk1:0.9 nM (Ki) Chk1:<1 nM (IC50) Chk2:8 nM (IC50) |
| In Vitro | Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is an ATP competitive CHK1 inhibitor, with a Ki of 0.9 nM and an IC50 of <1 nM[1]. Prexasertib (LY2606368) shows high anti-tumor activity against U-2 OS, Calu-6 and HeLa cells (IC50, 3, 3, 37 nM, respectively), causes DNA damage during S-phase requiring CDC25A and CDK2 at 4 μM[1]. Prexasertib (0-20 nM) synergizes with olaparib (0-20 μM) to decrease cell viability in HGSOC cells[2]. |
| Animal Admin | Prexasertib (1, 3.3 or 10 mg/kg s.c.) is well tolerated, and significantly inhibits tumor inhibition in mice bearing Calu-6 xenograft tumors[1]. |
| References |
| Molecular Formula | C19H25N7O6S |
|---|---|
| Molecular Weight | 479.51 |
| Storage condition | 2-8℃ |