BAG-956 | NVP-BAG956 | CAS#853910-02-8 | PI 3-kinase Inhibitor

MedKoo Cat#: 524364 | Name: BAG-956

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

BAG 956, also known as NVP-BAG956, is a dual PDK1 and class I PI 3-kinase inhibitor. BAG 956 has been shown to inhibit cellular AKT phosphorylation at Thr308. BAG 956 also blocks cell proliferation and causes arrest in the G1 phase of the cell cycle. BAG 956 has been shown to slow tumor progression in mouse xenograft models.

Chemical Structure

BAG-956

CAS#853910-02-8

Theoretical Analysis

MedKoo Cat#: 524364

Name: BAG-956

CAS#: 853910-02-8

Chemical Formula: C28H21N5

Exact Mass: 427.1800

Molecular Weight: 427.51

Elemental Analysis: C, 78.67; H, 4.95; N, 16.38

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 350.00	2 Weeks
10mg	USD 650.00	2 Weeks

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Related CAS #

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Synonym

BAG-956; BAG 956; BAG956; NVP-BAG956; NVP-BAG-956; NVP-BAG 956.

IUPAC/Chemical Name

α,α-dimethyl-4-[2-methyl-8-[2-(3-pyridinyl)ethynyl]-1H-imidazo[4,5-c]quinolin-1-yl]-benzeneacetonitrile

InChi Key

GVPAGJWVBUZHNQ-UHFFFAOYSA-N

InChi Code

InChI=1S/C28H21N5/c1-19-32-26-17-31-25-13-8-20(6-7-21-5-4-14-30-16-21)15-24(25)27(26)33(19)23-11-9-22(10-12-23)28(2,3)18-29/h4-5,8-17H,1-3H3

SMILES Code

N#CC(C)(C)C1=CC=C(N2C(C)=NC3=C2C4=CC(C#CC5=CC=CN=C5)=CC=C4N=C3)C=C1

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, 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

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

NVP-BAG956 is a PI3K inhibitor with IC50s of 34, 56, 112 and 444 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.

In vitro activity:

Treatment of MOLM14 for 24 hours with 250 and 500 nM BAG956 caused significant cell-cycle (G1) arrest (42.693% G1 in control; 80.748% G1 in 250 nM BAG956-treated; 77.981% G1 in 500 nM BAG956-treated; Figure S2A). Treatment of MOLM14 cells for 72 hours with 250 and 500 nM BAG956 led to an induction of apoptosis (93.2% viable/6.7% apoptotic control cells; 77.5% viable/22.4% apoptotic for 250 nM BAG956-treated cells; 63.9% viable/35% apoptotic for 500 nM BAG956-treated cells; Figure S3A). These data suggest that BAG956 is both cytostatic and cytotoxic in nature. Reference: Blood. 2008 Apr 1;111(7):3723-34. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2275029/

In vivo activity:

Effects of BAG956 were investigated in vivo alone (at a dose of 100 mg/kg) and in combination with nilotinib (at a dose of 20 mg/kg) using mice IV injected with 32D.p210-luc+ cells. Overall tumor burden, as assessed by measured levels of bioluminescence in vehicle- and drug-treated mice, was observed to be the lowest in the BAG956 (100 mg/kg) + nilotinib (20 mg/kg)-treated group, compared with mice treated with vehicle or either agent alone (Figure 6A,B). At the time of death, there was no significant difference in percentage of spleen/total weights observed between vehicle- and drug-treated mice (Figure S9). For the last imaging day (day 9 after intravenous injection), Student t test was used for statistical evaluation of differences in bioluminescence and yielded: P ≤ .049 (vehicle vs nilotinib), P ≤ .595 (vehicle vs BAG956), P ≤ .006 (vehicle vs drug combination), P ≤ .006 (drug combination vs nilotinib), and P ≤ .222 (drug combination vs BAG956). Reference: Blood. 2008 Apr 1;111(7):3723-34. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2275029/

	Solvent	mg/mL	mM
Solubility
	DMSO	18.6	44.27
	Ethanol	8.6	20.41

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 427.51 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Weisberg E, Banerji L, Wright RD, Barrett R, Ray A, Moreno D, Catley L, Jiang J, Hall-Meyers E, Sauveur-Michel M, Stone R, Galinsky I, Fox E, Kung AL, Griffin JD. Potentiation of antileukemic therapies by the dual PI3K/PDK-1 inhibitor, BAG956: effects on BCR-ABL- and mutant FLT3-expressing cells. Blood. 2008 Apr 1;111(7):3723-34. doi: 10.1182/blood-2007-09-114454. Epub 2008 Jan 9. PMID: 18184863; PMCID: PMC2275029.

In vitro protocol:

In vivo protocol:

1: Bressanin D, Evangelisti C, Ricci F, Tabellini G, Chiarini F, Tazzari PL, Melchionda F, Buontempo F, Pagliaro P, Pession A, McCubrey JA, Martelli AM. Harnessing the PI3K/Akt/mTOR pathway in T-cell acute lymphoblastic leukemia: eliminating activity by targeting at different levels. Oncotarget. 2012 Aug;3(8):811-23. PubMed PMID: 22885370; PubMed Central PMCID: PMC3478458. 2: Marone R, Erhart D, Mertz AC, Bohnacker T, Schnell C, Cmiljanovic V, Stauffer F, Garcia-Echeverria C, Giese B, Maira SM, Wymann MP. Targeting melanoma with dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors. Mol Cancer Res. 2009 Apr;7(4):601-13. doi: 10.1158/1541-7786.MCR-08-0366. PubMed PMID: 19372588. 3: Weisberg E, Banerji L, Wright RD, Barrett R, Ray A, Moreno D, Catley L, Jiang J, Hall-Meyers E, Sauveur-Michel M, Stone R, Galinsky I, Fox E, Kung AL, Griffin JD. Potentiation of antileukemic therapies by the dual PI3K/PDK-1 inhibitor, BAG956: effects on BCR-ABL- and mutant FLT3-expressing cells. Blood. 2008 Apr 1;111(7):3723-34. doi: 10.1182/blood-2007-09-114454. Epub 2008 Jan 9. PubMed PMID: 18184863; PubMed Central PMCID: PMC2275029.