BAY1082439
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MedKoo CAT#: 205923

CAS#: 1375469-38-7

Description: BAY1082439 is an orally bioavailable inhibitor of the class I phosphoinositide 3-kinase (PI3K) alpha and beta isoforms with potential antineoplastic activity. PI3K alpha/beta inhibitor BAY1082439 selectively inhibits both PI3K alpha, including mutated forms of PIK3CA, and PI3K beta in the PI3K/Akt/mTOR pathway, which may result in tumor cell apoptosis and growth inhibition in PI3K-expressing and/or PTEN-driven tumor cells. By specifically targeting class I PI3K alpha and beta, this agent may be more efficacious and less toxic than pan PI3K inhibitors.


Price and Availability

Size Price Shipping out time Quantity
5mg USD 90 Same Day
10mg USD 150 Same Day
25mg USD 250 Same Day
50mg USD 450 Same Day
100mg USD 750 Same Day
200mg USD 1250 Same Day
500mg USD 2050 Same Day
1g USD 3650 Same day
2g USD 5650 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-08-12. Prices are subject to change without notice.

BAY1082439, purity > 98%, is in stock. The same day shipping out after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 205923
Name: BAY1082439
CAS#: 1375469-38-7
Chemical Formula: C25H30N6O5
Exact Mass: 494.2278
Molecular Weight: 494.552
Elemental Analysis: C, 60.72; H, 6.11; N, 16.99; O, 16.18


Synonym: BAY10-82439; BAY 10-82439; BAY-10-82439; BAY1082439; BAY 1082439; BAY-1082439.

IUPAC/Chemical Name: (S)-N-(8-(2-hydroxy-3-morpholinopropoxy)-7-methoxy-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl)-2-methylnicotinamide

InChi Key: JGNRMIWLBBNSMU-KRWDZBQOSA-N

InChi Code: InChI=1S/C25H30N6O5/c1-16-18(4-3-7-26-16)24(33)29-25-28-21-19(23-27-8-9-31(23)25)5-6-20(22(21)34-2)36-15-17(32)14-30-10-12-35-13-11-30/h3-7,17,32H,8-15H2,1-2H3,(H,28,29,33)/t17-/m0/s1

SMILES Code: C1=CC(OC[C@@H](O)CN2CCOCC2)=C(OC)C2N=C(NC(=O)C3=CC=CN=C3C)N3CCN=C3C1=2


Technical Data

Appearance:
White to off-white solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Safety Data Sheet (SDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001


Additional Information

BAY1082439 is a highly selective PI3Kα/α-balanced inhibitor. BAY 1082439 represents a new type of PI3K inhibitor with unique pharmacological and pharmacodynamic properties. BAY 1082439 has an IC50 ratio of 1:3 in biochemical assays of PI3Kα (4.9 nM) vs. PI3Kα (15.0 nM), and >1000-fold selectivity against mTOR kinase. In vivo, BAY 1082439 showed clear advantages over the strong PI3Kα inhibitor BAY 80-6946 in PTEN/PI3Kα-driven tumor models (e.g., PC3 and HEC-1B), when the two compounds were compared at their MTDs. Furthermore, BAY 1082439 has unique pharmacokinetic (PK) properties with very high plasma free fractions across all species tested (33-50%), large Vss, high clearance and intermediate T1/2.   BAY 1082439 showed strong p-AKT inhibition at 2 and 5 hours post-treatment while p-AKT returned to levels comparable to the vehicle group at 24 hours in all 4 tumor models tested. Interestingly, with once daily dosing, BAY 1082439 could induce tumor regression in KPL4 (PIK3CAmut and HER2+), and tumor stasis in HEC-1B (PTENdel) and in HEC-1A (PIK3CAmut) tumor models. (source:  Cancer Research: April 15, 2012; Volume 72, Issue 8, Supplement 1 doi: 10.1158/1538-7445.AM2012-2799. Proceedings: AACR 103rd Annual Meeting 2012-- Mar 31-Apr 4, 2012; Chicago, IL )   
 
 
 


References