Product Name :
Tenalisib
Description:
Tenalisib (RP6530) is a novel, potent, and selective PI3Kδ and PI3Kγ inhibitor with IC50 values of 25 and 33 nM, respectively.
CAS:
1639417-53-0
Molecular Weight:
415.42
Formula:
C23H18FN5O2
Chemical Name:
3-(3-fluorophenyl)-2-[(1S)-1-[(7H-purin-6-yl)amino]propyl]-4H-chromen-4-one
Smiles :
CC[C@H](NC1N=CN=C2N=CNC=12)C1OC2=CC=CC=C2C(=O)C=1C1C=C(F)C=CC=1
InChiKey:
HDXDQPRPFRKGKZ-INIZCTEOSA-N
InChi :
InChI=1S/C23H18FN5O2/c1-2-16(29-23-19-22(26-11-25-19)27-12-28-23)21-18(13-6-5-7-14(24)10-13)20(30)15-8-3-4-9-17(15)31-21/h3-12,16H,2H2,1H3,(H2,25,26,27,28,29)/t16-/m0/s1
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.Insulin (swine) Epigenetics
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.Tucatinib Cancer
Additional information:
Tenalisib (RP6530) is a novel, potent, and selective PI3Kδ and PI3Kγ inhibitor with IC50 values of 25 and 33 nM, respectively.|Product information|CAS Number: 1639417-53-0|Molecular Weight: 415.42|Formula: C23H18FN5O2|Chemical Name: 3-(3-fluorophenyl)-2-[(1S)-1-[(7H-purin-6-yl)amino]propyl]-4H-chromen-4-one|Smiles: CC[C@H](NC1N=CN=C2N=CNC=12)C1OC2=CC=CC=C2C(=O)C=1C1C=C(F)C=CC=1|InChiKey: HDXDQPRPFRKGKZ-INIZCTEOSA-N|InChi: InChI=1S/C23H18FN5O2/c1-2-16(29-23-19-22(26-11-25-19)27-12-28-23)21-18(13-6-5-7-14(24)10-13)20(30)15-8-3-4-9-17(15)31-21/h3-12,16H,2H2,1H3,(H2,25,26,27,28,29)/t16-/m0/s1|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : ≥ 100 mg/mL (240.72 mM).|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|Tenalisib shows selectivity over PI3K α (>300-fold) and β (>100-fold) isoforms.PMID:33301050 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.|Products are for research use only. Not for human use.|