Tenalisib
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 100mg | $550 | Check With Us |
| 250mg | $1100 | Check With Us |
| 500mg | $1650 | Check With Us |
: Cat #: V3107 CAS #: 1639417-53-0 Purity ≥ 98%
Description: Tenalisib (also known as RP6530) is a new, potent and selective dual PI3Kδ/γ inhibitor with anticancer activity.
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- Physicochemical and Storage Information
- Protocol
- Related Biological Data
- Stock Solution Preparation
- Quality Control Documentation
| Molecular Weight (MW) | 415.42 |
|---|---|
| Molecular Formula | C23H18FN5O2 |
| CAS No. | 1639417-53-0 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 10 mMr |
| Water: N/Ar | |
| Ethanol: N/A | |
| SMILES Code | O=C1C(C2=CC=CC(F)=C2)=C([C@@H](NC3=C4NC=NC4=NC=N3)CC)OC5=CC=CC=C15 |
| Synonyms | RP-6530; RP6530; RP 6530 |
| Protocol | In Vitro | Tenalisib shows selectivity over PI3K α (>300-fold) and β (>100-fold) isoforms. Tenalisib exhibits modest proliferation inhibition (33-46% inhibition @ 10 μM) in both HEL-RS and HEL-RR cells. Addition of 10 μM tenalisib to ruxolitinib is synergistic resulting in a near-complete inhibition of proliferation (>90% for HEL-RS and >70% for HEL-RR). Addition of 5 μM tenalisib, 4 h prior to the addition of ruxolitinib results in a significant reduction in EC50of ruxolitinib (5.8 μM) in HEL-RR cells. Incubation of 10 μM tenalisib with ruxolitinib for 72 h increases the percent of apoptotic cells (55% in HEL-RS and 37% in HEL-RR) compared to either agent alone (16-27% in HEL-RS and 17-21% in HEL-RR). |
|---|---|---|
| In Vivo | Tenalisib has been well tolerated in subjects with heavily pre-treated relapsed/refractory hematologic malignancies. Reported toxicities are manageable with no DLTs. Single agent activity is evident in difficult-to-treat subjects at ≥ 200 mg BID. |
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 | 2.4072 mL | 12.0360 mL | 24.0720 mL | 48.1440 mL |
| 5mM | 0.4814 mL | 2.4072 mL | 4.8144 mL | 9.6288 mL |
| 10mM | 0.2407 mL | 1.2036 mL | 2.4072 mL | 4.8144 mL |
| 20mM | 0.1204 mL | 0.6018 mL | 1.2036 mL | 2.4072 mL |
The molarity calculator equation
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The dilution calculator equation
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Step One: Enter information below
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Step Two: Enter the in vivo formulation
%DMSO
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%
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%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
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Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
µL
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mg/mL)
,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:
Take
µL
DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (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.