Home Categories Pharmaceutical intermediates BYL719
A1407812

BYL719 , 98% , 1217486-61-7

CAS NO.:1217486-61-7

Empirical Formula: C19H22F3N5O2S

Molecular Weight: 441.47

MDL number: MFCD22417085

Pack Size Price Stock Quantity
1mg RMB199.20 In Stock
5MG RMB594.40 In Stock
10MG RMB1095.20 In Stock
20MG RMB1439.20 In Stock
50MG RMB2983.20 In Stock
100mg RMB4665.60 In Stock
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Update time: 2022-07-08

PRODUCT Properties

Density  1.391
storage temp.  Store at -20°C
solubility  ≥22.07 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
form  White solid.
pka 6.29±0.70(Predicted)
color  Off-white to light yellow
InChIKey STUWGJZDJHPWGZ-LBPRGKRZSA-N
SMILES N1(C(NC2=NC(C)=C(C3C=CN=C(C(C)(C)C(F)(F)F)C=3)S2)=O)CCC[C@H]1C(N)=O

Description and Uses

BYL719 is an inhibitor of phosphoinositide 3-kinase α (PI3Kα; IC50s = 4.6, 4, and 4.8 nM for wild-type, E545K mutant, and H1047R mutant PI3K, respectively). It is selective for PI3Kα over PI3Kβ, PI3Kδ, PI3Kγ, and PI4Kβ (IC50s = 1,156, 290, 250, and 581 nM, respectively), as well as VPS34, mTOR, DNA-PK, and ATR (IC50s = >9,100 nM for all). BYL719 (12.5, 25, and 50 mg/kg) reduces tumor volume in a PI3Kα-dependent Rat1-myr-p110α mouse xenograft model. It also reduces tumor burden in THP-1 acute myeloid leukemia (AML) and MCF-7 breast cancer mouse xenograft models. Formulations containing BYL719 have been used in the treatment of advanced or metastatic breast cancer.

(2S)-N1-[4-Methyl-5-[2-(2,2,2-trifluoro-1,1-dimethylethyl)-4-pyridinyl]-2-thiazolyl]-1,2-pyrrolidinedicarboxamide is a newly developed phosphatidylinositol-3-kinase (PI3K) inhibitor and a mTOR inhibitor for the treatment of proliferative diseases.

Safety

Symbol(GHS) 
GHS08
Signal word  Danger
Hazard statements  H373
Precautionary statements  P260-P314-P501
HS Code  29341000

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