BYL719 1217486-61-7

.cp_wz table {border-top: 1px solid #ccc;border-left:1px solid #ccc; } .cp_wz table td{border-right: 1px solid #ccc; border-bottom: 1px solid #ccc; padding: 5px 0px 0px 5px;} .cp_wz table th {border-right: 1px solid #ccc;border-bottom: 1px solid #ccc; padding: 5px 0px 0px 5px;}


Molecular Weight: 441.47 BYL719 is a potent and selective PI3Kα inhibitor with IC50 of 5 nM, and minimal effect on PI3Kβ/γ/δ. Phase 2.

BYL719 inhibits the proliferation of breast cancer cell lines harboring
PIK3CA mutations, correlating with inhibition of various downstream
signaling components of the PI3K/Akt pathway.



BYL719(>270 mg/d) shows statistically significant dose-dependent
anti-tumor efficacy in PIK3CA mutant xenograft models in rodents. BYL719
has a low clearance, a half-life of 8.5 h and its exposure increases
dose proportionally between 30mg/d and 450mg/d, displaying a low
inter-individual variability in Cmax and AUC in human. BYL719(270mg/d)
shows first signs of clinical efficacy include 1 confirmed partial
response in a patient with ER+ breast cancer, and significant PET
responses (PMR) and/or tumor shrinkage are achieved in 8 out of 17
evaluated patients.


Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Chemical Information

Molecular Weight (MW)	441.47
Formula	C19H22F3N5O2S
CAS No.	1217486-61-7

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms

Solubility (25°C) *	In vitro	DMSO	88 mg/mL (199.33 mM)
		Water	<1 mg/mL (
		Ethanol	2 mg/mL (4.53 mM)
	In vivo	30% PEG400/0.5% Tween80/5% propylene glycol	30 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Name	1,2-Pyrrolidinedicarboxamide, N1-[4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethylethyl)-4-pyridinyl]-2-thiazolyl]-, (2S)-

Molarity Calculator
Dilution Calculator
Molecular Weight Calculator

Contact us if you need more details on BYL719 1217486-61-7. We are ready to answer your questions on packaging, logistics, certification or any other aspects about 1217486-61-7 BYL719、1217486-61-7. If these products fail to match your need, please contact us and we would like to provide relevant information.

Product Categories : PI3K/Akt/mTOR > PI3K Inhibitor