NVP-BHG712 isomer

NVP-BHG712 isomer - Names and Identifiers

Name	4-methyl-3-((2-methyl-6-(pyridin-3-yl)-2H-pyrazolo[3,4-d]pyrimidin-4-yl)amino)-N-(3-(trifluoromethyl)phenyl)benzamide
Synonyms	NVP-BHG712 isomer 4-methyl-3-((2-methyl-6-(pyridin-3-yl)-2H-pyrazolo[3,4-d]pyrimidin-4-yl)amino)-N-(3-(trifluoromethyl)phenyl)benzamide
CAS	2245892-85-5

NVP-BHG712 isomer - Physico-chemical Properties

Molecular Formula	C26H20F3N7O
Molar Mass	503.48
Solubility	DMSO : 25 mg/mL mother liquor preservation: sub-package and freeze storage to avoid repeated freezing and thawing;-20 ℃,1 month;-80 ℃,6 months (after dilution, the solution temperature is low and storage may precipitate, try to use it now) Cell experiment: Dissolve with DMSO first: dilute with culture medium then, and the dilution process is recommended to be carried out in stages to avoid too fast concentration change leading to compound precipitation. If the compound is precipitated during the dilution process, it can be redissolved by ultrasound. During dilution, ensure that the final concentration of DMSO in the working fluid should be below 0.1% as far as possible, and the maximum should not exceed 0.5%, and set up a DMSO control group with corresponding concentration. Animal experiment: Dissolve with DMSO first: dilute with water or normal saline, etc. The dilution process is recommended to be carried out in sections to avoid excessive concentration changes leading to compound p
Storage Condition	-20℃
Use	NVP-BHG712 isomer is a regioisomer of NVP-BHG712, which shows conserved non-bonded binding to EPHA2 and EPHB4. BHG-712, is a EphB4 kinase inhibitor and BCR-ABL inhibitor. NVP-BHG712 inhibits EphB4 kinase activity in the low nanomolar range in cellular assays showed high selectivity for targeting the EphB4 kinase when profiled against other kinases in biochemical as well as in cell based assays. BHG-712 shows excellent pharmacokinetic properties and potently inhibits EphB4 autophosphorylation in tissues after oral administration.
Target	EPHA2
In vitro study	NVP-BHG712 isomer exhibits IC 50 values of 163 nM and 1660 nM for EPHA2 and EPHA4, respectively.

NVP-BHG712 isomer - Reference

Reference

1: Li T, Wang H, Liu R, Wang X, Huang L, Wu Z, Yin X, Zou S, Duan P. The role of EphB4/ephrinB2 signaling in root repair after orthodontically-induced root resorption. Am J Orthod Dentofacial Orthop. 2021 Mar;159(3):e217-e232. doi: 10.1016/j.ajodo.2020.07.035. Epub 2021 Jan 22. PMID: 33487501.
2: Neuber C, Tröster A, Löser R, Belter B, Schwalbe H, Pietzsch J. The Pyrazolo[3,4-d]pyrimidine-Based Kinase Inhibitor NVP-BHG71
2: Effects of Regioisomers on Tumor Growth, Perfusion, and Hypoxia in EphB4-Positive A375 Melanoma Xenografts. Molecules. 2020 Nov 3;25(21):5115. doi: 10.3390/molecules25215115. PMID: 33153234; PMCID: PMC7662635.
3: Broggini T, Piffko A, Hoffmann CJ, Ghori A, Harms C, Adams RH, Vajkoczy P, Czabanka M. Ephrin-B2-EphB4 communication mediates tumor-endothelial cell interactions during hematogenous spread to spinal bone in a melanoma metastasis model. Oncogene. 2020 Nov;39(47):7063-7075. doi: 10.1038/s41388-020-01473-y. Epub 2020 Sep 28. PMID: 32989254.
4: Wan X, Saban DV, Kim SN, Weng Y, Dammann P, Keyvani K, Sure U, Zhu Y. PDCD10-Deficiency Promotes Malignant Behaviors and Tumor Growth via Triggering EphB4 Kinase Activity in Glioblastoma. Front Oncol. 2020 Aug 7;10:1377. doi: 10.3389/fonc.2020.01377. PMID: 32850441; PMCID: PMC7427606.
5: Andolfo I, Lasorsa VA, Manna F, Rosato BE, Formicola D, Iolascon A, Capasso M. Kinome multigenic panel identified novel druggable EPHB4-V871I somatic variant in high-risk neuroblastoma. J Cell Mol Med. 2020 Jun;24(11):6459-6471. doi: 10.111

NVP-BHG712 isomer - Preparation solution concentration reference

	1mg	5mg	10mg
1 mM	1.987 ml	9.937 ml	19.874 ml
5 mM	0.397 ml	1.987 ml	3.975 ml
10 mM	0.199 ml	0.994 ml	1.987 ml
5 mM	0.04 ml	0.199 ml	0.397 ml

Last Update：2024-01-02 23:10:35

NVP-BHG712 isomer - Reference Information

biological activity	NVP-BHG712 isomer, a NVP-BHG712 positional isomer that shows conservative non-bond binding to EPHA2 and ephb4.
Target	IC50: 163 nM (EPHA2).

Last Update：2024-04-09 20:52:54