BAY-1125976
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MedKoo CAT#: 407996

CAS#: 1402608-02-9

Description: BAY-1125976 is a potent and selective allosteric AKT1/2 inhibitor. BAY-1125976 exhibits high efficacy on AKT signaling-dependent tumor growth in mouse models. BAY 1125976 potently and selectively inhibited the activity of full-length AKT1 and AKT2 by binding into an allosteric binding pocket formed by kinase and PH domain. In vitro, BAY 1125976 inhibited cell proliferation in a broad panel of human cancer cell lines. BAY 1125976 exhibited strong in vivo efficacy in both cell line and patient-derived xenograft models such as the KPL4 breast cancer model (PIK3CAH1074R mutant), the MCF7 and HBCx-2 breast cancer models and the AKTE17K mutant driven prostate cancer (LAPC-4) and anal cancer (AXF 984) models.


Price and Availability

Size
Price

25mg
USD 250
200mg
USD 1250
2g
USD 5250
Size
Price

50mg
USD 450
500mg
USD 1950
Size
Price

100mg
USD 750
1g
USD 2950

BAY-1125976, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 407996
Name: BAY-1125976
CAS#: 1402608-02-9
Chemical Formula: C23H21N5O
Exact Mass: 383.1746
Molecular Weight: 383.45
Elemental Analysis: C, 72.04; H, 5.52; N, 18.26; O, 4.17


Synonym: BAY-1125976; BAY 1125976; BAY1125976;

IUPAC/Chemical Name: Imidazo[1,2-b]pyridazine-6-carboxamide, 2-[4-(1-aminocyclobutyl)phenyl]-3-phenyl-

InChi Key: JBGYKRAZYDNCNV-UHFFFAOYSA-N

InChi Code: InChI=1S/C23H21N5O/c24-22(29)18-11-12-19-26-20(21(28(19)27-18)16-5-2-1-3-6-16)15-7-9-17(10-8-15)23(25)13-4-14-23/h1-3,5-12H,4,13-14,25H2,(H2,24,29)

SMILES Code: O=C(C1=NN2C(C=C1)=NC(C3=CC=C(C4(N)CCC4)C=C3)=C2C5=CC=CC=C5)N


Technical Data

Appearance:
Solid powder

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

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

Shelf Life:
>3 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).

Harmonized System Code:
2934990300


Additional Information

The PI3K-AKT-mTOR signaling cascade is activated in the majority of human cancers, and its activation also plays a key role in resistance to chemo and targeted therapeutics. In particular, in both breast and prostate cancer, increased AKT pathway activity is associated with cancer progression, treatment resistance and poor disease outcome.


References

1: Politz O, Siegel F, Bärfacker L, Bömer U, Hägebarth A, Scott WJ, Michels M,
Ince S, Neuhaus R, Meyer K, Fernández-Montalván AE, Liu N, von Nussbaum F,
Mumberg D, Ziegelbauer K. BAY 1125976, a selective allosteric AKT1/2 inhibitor,
exhibits high efficacy on AKT signaling-dependent tumor growth in mouse models.
Int J Cancer. 2017 Jan 15;140(2):449-459. doi: 10.1002/ijc.30457. Epub 2016 Oct
20. PubMed PMID: 27699769.