Cart
sales@molnova.com
Tenalisib (RP6530)
CAS No. 1639417-53-0
Tenalisib (RP6530) ( RP6530 )
Catalog No. M21860 CAS No. 1639417-53-0
Tenalisib (RP6530) is a novel, potent, and selective PI3Kδ and PI3Kγ inhibitor with IC50 values of 25 and 33 nM, respectively.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 2MG | 41 | In Stock |
|
| 5MG | 67 | In Stock |
|
| 10MG | 102 | In Stock |
|
| 25MG | 178 | In Stock |
|
| 50MG | 288 | In Stock |
|
| 100MG | 434 | In Stock |
|
| 200MG | Get Quote | In Stock |
|
| 500MG | Get Quote | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
-
Product NameTenalisib (RP6530)
-
NoteResearch use only, not for human use.
-
Brief DescriptionTenalisib (RP6530) is a novel, potent, and selective PI3Kδ and PI3Kγ inhibitor with IC50 values of 25 and 33 nM, respectively.
-
DescriptionTenalisib shows selectivity over PI3K α (>300-fold) and β (>100-fold) isoforms. Tenalisib exhibits modest proliferation inhibition 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).
-
SynonymsRP6530
-
PathwayPI3K/Akt/mTOR signaling
-
TargetPI3K
-
RecptorPI3Kδ,PI3Kγ
-
Research Area——
-
Indication——
Chemical Information
-
CAS Number1639417-53-0
-
Formula Weight415.42
-
Molecular FormulaC23H18FN5O2
-
Purity>98% (HPLC)
-
SolubilityDMSO : ≥ 100 mg/mL (240.72 mM)
-
SMILESO=C1C(C2=CC=CC(F)=C2)=C([C@@H](NC3=C4NC=NC4=NC=N3)CC)OC5=CC=CC=C15
-
Chemical Name——
Shipping & Storage Information
-
Storage(-20℃)
-
ShippingWith Ice Pack
-
Stability≥ 2 years
Reference
1. Vakkalanka S, et al. RP6530, a dual PI3K δ/γ inhibitor, potentiates ruxolitinib activity in the JAK2-V617F mutant erythroleukemia cell lines. [abstract]. In: Proceedings of the 106th Annual Meeting of the American Association for Cancer Research; 2015 Apr 18-22; Philadelphia, PA. Philadelphia (PA): AACR; Cancer Res 2015;75(15 Suppl):Abstract nr 2704. doi:10.1158/1538-7445.AM2015-2704
2. Carmelo C, et al. A Dose Escalation Study of RP6530, a Novel Dual PI3K Delta/Gamma Inhibitor, in Patients with Relapsed/Refractory Hematologic Malignancies. Blood 2015 126:1495;
molnova catalog
related products
-
Vps34-IN-1
Vps34-IN-1 is a potent, selective inhibitor of class III PI3K Vps34 with IC50 of 25 nM.
-
PI3K/mTOR Inhibitor-...
PI3K/mTOR Inhibitor-2 is a potent pan inhibitor of PI3K and mTOR with IC50s of 3.4, 34, 16,1 and 4.7 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR. PI3K/mTOR Inhibitor-2 has antitumor activity.
-
PI-103 hydrochloride
A potent, dual class I PI3K/mTOR inhibitor with IC50 of 2/3/3/15/ for p110α/β/δ/γ, respectively.
