CRT 0066101
This product is for research use only, not for human use. We do not sell to patients.
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| Size | Price | Stock |
|---|---|---|
| 250mg | $1250 | Check With Us |
| 500mg | $1950 | Check With Us |
| 1g | $2925 | Check With Us |
: Cat #: V11937 CAS #: 1883545-60-5 Purity ≥ 98%
Description: CRT 0066101 is a novel, potent and selective inhibitor of protein kinase D (PKD) with IC50 values of 1, 2.5 and 2 nM for PKD1, 2, and 3 respectively.
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| Molecular Weight (MW) | 411.33 |
|---|---|
| Molecular Formula | C18H24Cl2N6O |
| CAS No. | 1883545-60-5 |
| Protocol | In Vitro | CRT0066101 specifically blocks PKD1/2 activity and does not suppress PKCα/PKCβ/PKCε activity in multiple cancer cell types including A549 (lung) and MiaPaCa-2 (pancreas). CRT0066101 significantly inhibits Panc-1 cell proliferation with an IC50 value of 1 µM. Treatment with CRT0066101 results in a 6-10 fold induction of apoptosis in Panc-1 cells. CRT0066101 significantly reduces cell proliferation of Colo357, Panc-1, MiaPaCa-2, and AsPC-1 cells but has a modest effect in Capan-2 cells. CRT0066101 (5 µM) blocks both the basal and NT-induced pS916-PKD1/2 (activated PKD1/2) in Panc-1 and Panc-28 cells. CRT0066101 reduces PKD-dependent NF-κB activation and NF-κB-dependent gene expressions in Panc-1 |
|---|---|---|
| In Vivo | Optimal therapeutic concentrations (8 µM) of CRT0066101 are detectable 6 h after oral administration of this drug. CRT0066101 given orally (80 mg/kg/day) for 28 days significantly abrogates PaCa growth in Panc-1 subcutaneous xenograft model. Activated PKD1/2 expression in the treated tumor-explants is significantly inhibited with peak tumor concentration (12 µM) of CRT0066101 achieved within 2 h after oral administration. Further, CRT0066101 given orally (80 mg/kg/day) for 21 days in Panc-1 orthotopic model potently blocks tumor growth in vivo. CRT0066101 significantly reduces Ki-67+ proliferation index, increases TUNEL+ apoptotic cells (p<0.05), and abrogates expression of NF-κB-dependent proteins including cyclin D1, survivin, and cIAP-1 |
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 | 2.4311 mL | 12.1557 mL | 24.3114 mL | 48.6228 mL |
| 5mM | 0.4862 mL | 2.4311 mL | 4.8623 mL | 9.7246 mL |
| 10mM | 0.2431 mL | 1.2156 mL | 2.4311 mL | 4.8623 mL |
| 20mM | 0.1216 mL | 0.6078 mL | 1.2156 mL | 2.4311 mL |
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Method for preparing in vivo formulation:
Take
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µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
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