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| Size | Price | Stock |
|---|---|---|
| 2mg | $60 | In Stock |
| 5mg | $90 | In Stock |
| 10mg | $140 | In Stock |
| 25mg | $250 | In Stock |
| 50mg | $420 | In Stock |
| 100mg | $650 | In Stock |
| 250mg | $1150 | In Stock |
| 500mg | $1725 | In Stock |
: Cat #: V2965 CAS #: 1876467-74-1 freebase Purity ≥ 98%
Description: Elimusertib (formerly known as BAY-1895344) is a highly selective and orally bioavailable inhibitor of ATR (ataxia telangiectasia and Rad3-related) with potential anticancer activity. It inhibits ATR with an IC50 value of 7 nM. BAY 1895344 shows potent anti-proliferative activity in vitro against a broad spectrum of human cancer cell lines with an IC50 of 78 nM. It is being investigated in clinical trials for cancer treatment since 2017. In cellular mechanistic assays BAY 1895344 potently inhibited hydroxyurea-induced H2AX phosphorylation (IC50 = 36 nM). Moreover, BAY 1895344 revealed significantly improved aqueous solubility, bioavailability across species and no activity in the hERG patch-clamp assay. BAY 1895344 also demonstrated very promising efficacy in monotherapy in DNA damage deficient tumor models as well as combination treatment with DNA damage inducing therapies.
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| Molecular Weight (MW) | 375.43 |
|---|---|
| Molecular Formula | C20H22ClN7O |
| CAS No. | 1876467-74-1 freebase |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 5.4 mg/mL (14.38 mM |
| Need ultrasonic) | |
| N/A | |
| N/A | |
| Synonyms | BAY-1895344; Elimusertib; BAY 1895344; BAY1895344. |
| Protocol | In Vitro | In vitro activity: BAY-1895344 is a potent, highly selective and orally available ATR (ataxia telangiectasia and Rad3-related) inhibitor with an IC50 of 7 nM. In vitro, BAY 1895344 potently inhibits proliferation of a broad spectrum of human tumor cell lines (median IC50 = 78 nM). In cellular mechanistic assays BAY 1895344 potently inhibited hydroxyurea-induced H2AX phosphorylation (IC50 = 36 nM). Moreover, BAY 1895344 revealed significantly improved aqueous solubility, bioavailability across species and no activity in the hERG patch-clamp assay. BAY 1895344 also demonstrated very promising efficacy in monotherapy in DNA damage deficient tumor models as well as combination treatment with DNA damage inducing therapies. The start of clinical investigation of BAY 1895344 is planned for early 2017. Kinase Assay: BAY 1895344 is shown to be a very potent and highly selective ATR inhibitor (IC50 = 7 nM), which potently inhibits proliferation of a broad spectrum of human tumor cell lines (median IC50 = 78 nM). In cellular mechanistic assays BAY 1895344 potently inhibits hydroxyurea-induced H2AX phosphorylation (IC50 = 36 nM). Cell Assay: In cellular mechanistic assays BAY 1895344 potently inhibited hydroxyurea-induced H2AX phosphorylation (IC50 = 36 nM). |
|---|---|---|
| In Vivo | BAY 1895344 exhibits strong in vivo anti-tumor efficacy in monotherapy in a variety of xenograft models of different indications that are characterized by DDR deficiencies, inducing stable disease in ovarian and colorectal cancer or even complete tumor remission in mantle cell lymphoma models |
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.6636 mL | 13.3181 mL | 26.6361 mL | 53.2722 mL |
| 5mM | 0.5327 mL | 2.6636 mL | 5.3272 mL | 10.6544 mL |
| 10mM | 0.2664 mL | 1.3318 mL | 2.6636 mL | 5.3272 mL |
| 20mM | 0.1332 mL | 0.6659 mL | 1.3318 mL | 2.6636 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.