CCT245737 S-isomer
This product is for research use only, not for human use. We do not sell to patients.
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| Size | Price | Stock |
|---|---|---|
| 5mg | $140 | 3-6 Days |
| 10mg | $210 | 3-6 Days |
| 25mg | $360 | 3-6 Days |
| 50mg | $540 | 3-6 Days |
| 100mg | $815 | 3-6 Days |
| 250mg | $1400 | 3-6 Days |
| 500mg | $2020 | 3-6 Days |
: Cat #: V2735 CAS #: 1489389-23-2 Purity ≥ 98%
Description: CCT245737 S-enantiomer, the S-isomer of CCT-245737, is an orally available and selective ATP-competitive inhibitor of CHK1 (checkpoint kinase 1) with an IC50 of 30-220 nM.
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| Molecular Weight (MW) | 379.34 |
|---|---|
| Molecular Formula | C16H16F3N7O |
| CAS No. | 1489389-23-2 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 75 mg/mL (197.7 mM) |
| Water: <1 mg/mL | |
| Ethanol: 9 mg/mL (23.7 mM) | |
| Synonyms | CCT 245737 S-enantiomer; CCT245737 S-isomer; CCT-245737. |
| Protocol | In Vitro | In vitro activity: CCT245737 is a potent inhibitor of recombinant human CHK1 with IC50 of 1.4±0.3 nM (mean±SD, n = 3, EZ Reader II assay). There is > 1,000-fold selectivity for CHK1 versus the functionally important kinases CDK1 and CHK2 (IC50=1.26-2.44 and 9.03 μM, respectively), and at least a 90-fold selectivity against cross-reacting kinases such as ERK8, PKD1, RSK1 and 2. CCT245737 potently inhibits cellular CHK1 activity (IC50 30-220nM) and enhances gemcitabine and SN38 cytotoxicity in multiple human tumor cell lines and human tumor xenograft models. It can abrogate an etoposide-induced G2/M arrest. CCT245737 has high cell permeability, as measured by transport across a CaCo2 cell monolayer. Kinase Assay: CCT245737 shows<50% 10='' 121='' inhibition='' at='' m='' for='' representing='' a='' selectivity='' chk1='' of=''>5000-fold over these enzymes. Commercial in vitro 33P radiometric kinase assays are carried out against 124 human kinases using 10 μM CCT245737 at ATP concentrations corresponding to the kinase Km, ATP. Other kinase IC50 determinations for CHK2 and FLT3 are performed using a commercial assay or in-house with recombinant human CHK1 on a LabChip® EZ Reader II or CDK1 in a DELFIA assay. Cell Assay: Cytotoxicity is determined as the drug concentration that gave 50% inhibition of tumor cell proliferation (GI50) using a 96h (i.e. 4-doublings) Sulforhodamine B (SRB) assay. Inhibition of intracellular CHK1 activity is measured using a cell based ELISA for the abrogation of an etoposide induced G2 checkpoint (mitosis induction assay, MIA). |
|---|---|---|
| In Vivo | Mouse oral bioavailability is complete (100%) with extensive tumor exposure. CCT245737 shows significant single-agent activity against a MYC-driven mouse model of B-cell lymphoma. An i.v. dose of 10mg/kg CCT245737 into BALB/c mice gives a peak plasma concentration of 4μmol/L, with a half-life of 2.86h, an AUC0-∞ of 9.96μmol.h/L, a plasma clearance of 2.1L/h/kg and a large volume of distribution (0.19L). The equivalent oral dose gave an almost identical profile with an AUC0-∞ of 10.4μmol.h/L showing complete oral bioavailability (F = 105%). In a word, CCT245737 shows complete oral bioavailability with linear pharmacokinetics and high tumor/plasma ratios consistent with extensive tumor exposure. Adequate CCT245737 tumor drug exposure takes a significant antitumor activity. | |
| Animal model | BALB/c mice |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.6362 mL | 13.1808 mL | 26.3616 mL | 52.7232 mL |
| 5mM | 0.5272 mL | 2.6362 mL | 5.2723 mL | 10.5446 mL |
| 10mM | 0.2636 mL | 1.3181 mL | 2.6362 mL | 5.2723 mL |
| 20mM | 0.1318 mL | 0.6590 mL | 1.3181 mL | 2.6362 mL |
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