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CB 300919

Potential therapy for ovarian cancer CAS# 289715-28-2

CB 300919

Catalog No. BCC1456----Order now to get a substantial discount!

Product Name & Size Price Stock
CB 300919:5mg $282.00 In stock
CB 300919:10mg $479.00 In stock
CB 300919:25mg $1128.00 In stock
CB 300919:50mg $1974.00 In stock
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Chemical structure

CB 300919

3D structure

Chemical Properties of CB 300919

Cas No. 289715-28-2 SDF Download SDF
PubChem ID 9938280 Appearance Powder
Formula C32H34ClN7O2 M.Wt 584.11
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 100 mg/mL (171.20 mM)
H2O : < 0.1 mg/mL (insoluble)
*"≥" means soluble, but saturation unknown.
Chemical Name 4-[[7-chloro-3-methyl-2-[(4-methylpiperazin-1-yl)methyl]-4-oxoquinazolin-6-yl]methyl-prop-2-ynylamino]-N-(pyridin-3-ylmethyl)benzamide
SMILES CN1CCN(CC1)CC2=NC3=CC(=C(C=C3C(=O)N2C)CN(CC#C)C4=CC=C(C=C4)C(=O)NCC5=CN=CC=C5)Cl
Standard InChIKey LWTCFUSGPRGUBX-UHFFFAOYSA-N
Standard InChI InChI=1S/C32H34ClN7O2/c1-4-12-40(26-9-7-24(8-10-26)31(41)35-20-23-6-5-11-34-19-23)21-25-17-27-29(18-28(25)33)36-30(38(3)32(27)42)22-39-15-13-37(2)14-16-39/h1,5-11,17-19H,12-16,20-22H2,2-3H3,(H,35,41)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of CB 300919

DescriptionCB 300919 is a water-soluble analogue of CB30865; has a continuous exposure (96 h) growth inhibition IC50 value of 2 nM in human CH1 ovarian tumor xenograft. IC50 value: Target: Nampt

References:
[1]. Lockman JW, et al. Analogues of 4-[(7-Bromo-2-methyl-4-oxo-3H-quinazolin-6-yl)methylprop-2-ynylamino]-N-(3-pyridylmethyl)benzamide (CB-30865) as Potent Inhibitors of Nicotinamide Phosphoribosyltransferase (Nampt). J. Med. Chem., 2010, 53 (24), pp 8734-87 [2]. Bavetsias, V. et al. The Design and Synthesis of Water-Soluble Analogues of CB30865, a Quinazolin-4-one-Based Antitumor Agent. Journal of Medicinal Chemistry (2002), 45(17), 3692-3702.

CB 300919 Dilution Calculator

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CB 300919 Molarity Calculator

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Preparing Stock Solutions of CB 300919

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.712 mL 8.56 mL 17.1201 mL 34.2401 mL 42.8002 mL
5 mM 0.3424 mL 1.712 mL 3.424 mL 6.848 mL 8.56 mL
10 mM 0.1712 mL 0.856 mL 1.712 mL 3.424 mL 4.28 mL
50 mM 0.0342 mL 0.1712 mL 0.3424 mL 0.6848 mL 0.856 mL
100 mM 0.0171 mL 0.0856 mL 0.1712 mL 0.3424 mL 0.428 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on CB 300919

CB 300919 is a potential therapy for ovarian cancer. Preclinical data showed that this quinazoline-based compound CB 300919 has a continuous exposure (96 h) growth inhibition IC50 value of 2 nM in human CH1 ovarian tumor xenograft.

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References on CB 300919

Mesenchymal stromal cells (MSCs) induce ex vivo proliferation and erythroid commitment of cord blood haematopoietic stem cells (CB-CD34+ cells).[Pubmed:28231331]

PLoS One. 2017 Feb 23;12(2):e0172430.

A human bone marrow-derived mesenchymal stromal cell (MSCs) and cord blood-derived CD34+ stem cell co-culture system was set up in order to evaluate the proliferative and differentiative effects induced by MSCs on CD34+ stem cells, and the reciprocal influences on gene expression profiles. After 10 days of co-culture, non-adherent (SN-fraction) and adherent (AD-fraction) CD34+ stem cells were collected and analysed separately. In the presence of MSCs, a significant increase in CD34+ cell number was observed (fold increase = 14.68), mostly in the SN-fraction (fold increase = 13.20). This was combined with a significant increase in CD34+ cell differentiation towards the BFU-E colonies and with a decrease in the CFU-GM. These observations were confirmed by microarray analysis. Through gene set enrichment analysis (GSEA), we noted a significant enrichment in genes involved in heme metabolism (e.g. LAMP2, CLCN3, BMP2K), mitotic spindle formation and proliferation (e.g. PALLD, SOS1, CCNA1) and TGF-beta signalling (e.g. ID1) and a down-modulation of genes participating in myeloid and lymphoid differentiation (e.g. PCGF2) in the co-cultured CD34+ stem cells. On the other hand, a significant enrichment in genes involved in oxygen-level response (e.g. TNFAIP3, SLC2A3, KLF6) and angiogenesis (e.g. VEGFA, IGF1, ID1) was found in the co-cultured MSCs. Taken together, our results suggest that MSCs can exert a priming effect on CD34+ stem cells, regulating their proliferation and erythroid differentiation. In turn, CD34+ stem cells seem to be able to polarise the BM-niche towards the vascular compartment by modulating molecular pathways related to hypoxia and angiogenesis.

DESolution of CD and CB Macrocycles.[Pubmed:28339123]

Chemistry. 2017 Jun 27;23(36):8601-8604.

Supramolecular chemistry utilizing the macrocyclic hosts cyclodextrins (CDs) and cucurbit[n]urils (CB[n]s) is traditionally performed in aqueous media; however, their solubility is typically poor, especially for the family of CB[n]s. Through derivatization of these macrocycles their solubility can be augmented to enable enhanced solubility in water and in some organic solvents. The increase in solubility of these derivatized macrocycles allows for their use in a wider range of chemical environments and giving rise to myriad potential applications. The dissolution of parent CDs (alpha-, beta- and gamma-) and CB[n]s (n=6-8) in deep eutectic solvents (DES) is reported, showing dramatic enhanced solubility of the larger species in both families, CB[7] and CB[8] as well as beta- and gamma-CD, respectively. Furthermore, the host-guest properties are maintained in this new solvation medium.

Draft Genome Sequence of Archangium sp. Strain Cb G35.[Pubmed:28232451]

Genome Announc. 2017 Feb 23;5(8). pii: 5/8/e01678-16.

In an effort to explore myxobacterial natural product biosynthetic pathways, the draft genome sequence of Archangium sp. strain Cb G35 has been obtained. Analysis of the genome using antiSMASH predicts 49 natural product biosynthetic pathways. This genome will contribute to the investigation of myxobacterial secondary metabolite biosynthetic pathways.

Description

CB 300919 is a quinazoline-based antitumour agent with high activity in the CH1 human ovarian tumour xenograft. CB 300919 has a continuous exposure (96 h) growth inhibition IC50 value of 2 nM in human CH1 ovarian tumor xenograft.

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