[CAS NO. 1312445-63-8] BuparlisibHydrochloride

Name: BuparlisibHydrochloride
Brand: Arctom Scientific
SKU: AS938769

Ships within

Stock

Price

Qty

Total

$0.00

Please click "REQUEST A QUOTE" button if you need other sizes or custom synthesis

request a quote

If there is no stock, or you need other sizes or custom synthesis, please:

PRODUCTS SPECIFICATIONS [1312445-63-8]

Distributor

Catalog

AS938769

Brand

Arctom Scientific

CAS

1312445-63-8

DESCRIPTION [1312445-63-8]

Overview

MDL	MFCD22124511
Molecular Weight	446.85
Molecular Formula	C18H22ClF3N6O2
SMILES	NC(N=C1)=CC(C(F)(F)F)=C1C2=NC(N3CCOCC3)=NC(N4CCOCC4)=C2.[H]Cl

For research use only. We do not sell to patients.

51 Publications Citing Use of MCE

Summary

Buparlisib Hydrochloride (BKM120 Hydrochloride) is a pan-class I PI3K inhibitor, with IC ₅₀ of 52 nM/166 nM/116 nM/262 nM for p110α / p110β / p110δ / p110γ , respectively.

IC50 & Target

p110α

52 nM (IC ₅₀ )

p110α-H1047R

58 nM (IC ₅₀ )

p110α-E545K

99 nM (IC ₅₀ )

p110δ

116 nM (IC ₅₀ )

p110β

166 nM (IC ₅₀ )

p110γ

262 nM (IC ₅₀ )

Vps34

2.4 μM (IC ₅₀ )

mTOR

4.6 μM (IC ₅₀ )

In Vitro

Buparlisib (BKM120) exhibits 50-300 nM activity for class I PI3K’s, including the most common p110α mutants. Additionally, NVP-BKM120 exhibits lower potency against class III and class IV PI3K's, where 2, 5, >5, and >25 μM biochemical activity is observed for inhibition of VPS34, mTOR, DNAPK, and PI4K, respectively ^[1] . Buparlisib (BKM120) induces multiple myeloma (MM) cell apoptosis in both dose- and time-dependent manners. Buparlisib (BKM120) at concentrations ≥10 μM induces significant apoptosis in all tested MM cell lines at 24 h (P<0.05, compares with control). Therefore, 10 μM Buparlisib (BKM120) and 24-h treatment are chose in in the following experiments if not stated otherwise. Buparlisib (BKM120) treatment results in a dose-dependent growth inhibition in all tested MM cell lines. Buparlisib (BKM120) IC ₅₀ varies among tested MM cells. At 24 h treatment, IC ₅₀ for ARP-1, ARK, and MM.1R is between 1 and 10 μM, while IC ₅₀ for MM.1S is <1 μM, and IC ₅₀ for U266 is between 10 and 100 μM. In summary, Buparlisib (BKM120) treatment results in MM cell growth inhibition and apoptosis in dose- and time-dependent manners ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

In A2780 xenograft tumors, oral dosing of Buparlisib (BKM120) at 3, 10, 30, 60, and 100 mg/kg results in a dose dependent modulation of pAKT ^Ser473 . Partial inhibition of pAKT ^Ser473 is observed at 3 and 10 mg/kg, and near complete inhibition is observed at doses of 30, 60, or 100 mg/kg, respectively. Inhibition of pAKT (normalized to total AKT) tracked well with both plasma and tumor drug exposure ^[1] . Mice receiving Buparlisib (BKM120) (5 μM per kg per day for 15 days) treatment has significantly smaller tumor burdens as compare with control mice, which are measured as tumor volume (P<0.05) and level of circulating human kappa chain (P<0.05). In addition, Buparlisib (BKM120) treatment significantly prolongs the survival of tumor-bearing mice (P<0.05) ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01512251	University of California, San Francisco\|Novartis	BRAF Mutant Metastatic Melanoma	June 9, 2012	Phase 1\|Phase 2
NCT02159066	Pfizer	Melanoma	July 23, 2014	Phase 2
NCT01626209	Novartis Pharmaceuticals\|Novartis	Advanced Breast Cancer, Advanced Carcinomas With Squamous Cell Histology	July 2012	Phase 1
NCT02340780	Canadian Cancer Trials Group\|Novartis	Chronic Lymphocytic Leukemia	January 30, 2015	Phase 2
NCT01285466	Novartis Pharmaceuticals\|Novartis	Metastatic or Locally Advanced Solid Tumors	January 2011	Phase 1
NCT01589861	Institut Paoli-Calmettes	Breast Cancer	December 2011	Phase 1\|Phase 2
NCT02614508	Emory University\|Novartis	Recurrent Chronic Lymphocytic Leukemia\|Recurrent Small Lymphocytic Lymphoma\|Refractory Chronic Lymphocytic Leukemia\|Refractory Small Lymphocytic Lymphoma	January 2016	Phase 1
NCT01820325	Novartis Pharmaceuticals\|Novartis	Non-Small Cell Lunch Cancer	September 9, 2013	Phase 1
NCT01527877	Yonsei University	Head Neck Cancer Squamous Cell Metastatic\|Head Neck Cancer Squamous Cell Recurrent	September 2012	Phase 2
NCT01339442	Washington University School of Medicine\|National Cancer Institute (NCI)	Estrogen Receptor-positive Breast Cancer\|Recurrent Breast Cancer\|Stage IV Breast Cancer	November 14, 2011	Phase 1
NCT01396499	M.D. Anderson Cancer Center\|Novartis	Leukemia	July 2012	Phase 1
NCT01634061	Novartis Pharmaceuticals\|Novartis	Castration-resistant Prostate Cancer	September 2012	Phase 1
NCT01629615	SOLTI Breast Cancer Research Group\|Novartis Pharmaceuticals\|Dana-Farber Cancer Institute\|Stand Up To Cancer	Breast Cancer	June 2012	Phase 2
NCT01289041	Novartis Pharmaceuticals\|Novartis	Advanced Endometrial Cancer	February 2011	Phase 2
NCT02088684	Novartis Pharmaceuticals\|Novartis	Breast Cancer	May 19, 2014	Phase 1
NCT01363232	Array Biopharma, now a wholly owned subsidiary of Pfizer\|Array BioPharma	Advanced Solid Tumors\|Selected Solid Tumors	August 2011	Phase 1
NCT02113878	Dana-Farber Cancer Institute\|Novartis Pharmaceuticals	Carcinoma, Squamous Cell of Head and Neck\|HPV Positive Oropharyngeal Squamous Cell Carcinoma\|Hypopharyngeal Cancer\|Early Invasive Cervical Squamous Cell Carcinoma\|Carcinoma of Larynx\|Cancer of Nasopharynx	September 29, 2014	Phase 1
NCT01911325	Novartis Pharmaceuticals\|Novartis	Squamous Non-small Cell Lung Cancer	October 2013	Phase 1
NCT01349660	SCRI Development Innovations, LLC\|Novartis	Glioblastoma Multiforme	December 2011	Phase 1\|Phase 2
NCT01816984	University of Chicago\|National Cancer Institute (NCI)	Metastatic Squamous Neck Cancer With Occult Primary Squamous Cell Carcinoma\|Recurrent Metastatic Squamous Neck Cancer With Occult Primary\|Recurrent Salivary Gland Cancer\|Recurrent Squamous Cell Carcinoma of the Hypopharynx\|Recurrent Squamous Cell Carcinoma of the Larynx\|Recurrent Squamous Cell Carcinoma of the Lip and Oral Cavity\|Recurrent Squamous Cell Carcinoma of the Nasopharynx\|Recurrent Squamous Cell Carcinoma of the Oropharynx\|Recurrent Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity\|Recurrent Verrucous Carcinoma of the Larynx\|Recurrent Verrucous Carcinoma of the Oral Cavity\|Salivary Gland Squamous Cell Carcinoma\|Stage IV Squamous Cell Carcinoma of the Hypopharynx\|Stage IV Squamous Cell Carcinoma of the Nasopharynx\|Stage IVA Salivary Gland Cancer\|Stage IVA Squamous Cell Carcinoma of the Larynx\|Stage IVA Squamous Cell Carcinoma of the Lip and Oral Cavity\|Stage IVA Squamous Cell Carcinoma of the Oropharynx\|Stage IVA Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity\|Stage IVA Verrucous Carcinoma of the Larynx\|Stage IVA Verrucous Carcinoma of the Oral Cavity\|Stage IVB Salivary Gland Cancer\|Stage IVB Squamous Cell Carcinoma of the Larynx\|Stage IVB Squamous Cell Carcinoma of the Lip and Oral Cavity\|Stage IVB Squamous Cell Carcinoma of the Oropharynx\|Stage IVB Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity\|Stage IVB Verrucous Carcinoma of the Larynx\|Stage IVB Verrucous Carcinoma of the Oral Cavity\|Stage IVC Salivary Gland Cancer\|Stage IVC Squamous Cell Carcinoma of the Larynx\|Stage IVC Squamous Cell Carcinoma of the Lip and Oral Cavity\|Stage IVC Squamous Cell Carcinoma of the Oropharynx\|Stage IVC Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity\|Stage IVC Verrucous Carcinoma of the Larynx\|Stage IVC Verrucous Carcinoma of the Oral Cavity\|Tongue Cancer	May 2013	Phase 1\|Phase 2
NCT01155453	Novartis Pharmaceuticals\|Novartis	Advanced and Selected Solid Tumors	April 2010	Phase 1
NCT01719250	Mayo Clinic\|National Cancer Institute (NCI)	Recurrent Adult Diffuse Large Cell Lymphoma\|Recurrent Grade 3 Follicular Lymphoma\|Recurrent Mantle Cell Lymphoma\|Refractory Mantle Cell Lymphoma\|Transformed Recurrent Non-Hodgkin Lymphoma	December 2012	Early Phase 1
NCT01297491	Novartis Pharmaceuticals\|Novartis	Non-small Cell Lung Cancer	May 2011	Phase 2
NCT01737450	Centre Leon Berard\|National Cancer Institute, France\|Fondation ARC	Head and Neck Neoplasms\|Neoplasm Metastasis\|Recurrent Disease\|Progressive Disease	January 2013	Phase 2
NCT01610284	Novartis Pharmaceuticals\|Novartis	Breast Cancer	August 7, 2012	Phase 3
NCT01727128	Novartis Pharmaceuticals\|Novartis	Hepatic Impairment	October 2011	Phase 1
NCT01572727	Novartis Pharmaceuticals\|Novartis	Breast Cancer	August 2012	Phase 2\|Phase 3
NCT02049541	Kami Maddocks, MD\|Novartis\|Ohio State University Comprehensive Cancer Center	Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue\|Nodal Marginal Zone B-cell Lymphoma\|Recurrent Grade 1 Follicular Lymphoma\|Recurrent Grade 2 Follicular Lymphoma\|Recurrent Grade 3 Follicular Lymphoma\|Recurrent Mantle Cell Lymphoma\|Recurrent Marginal Zone Lymphoma\|Splenic Marginal Zone Lymphoma\|Waldenström Macroglobulinemia	July 21, 2014	Phase 1
NCT01816594	Novartis Pharmaceuticals\|Breast International Group\|German Breast Group\|SOLTI Breast Cancer Research Group\|Novartis	HER2-positive Newly Diagnosed, Primary Breast Cancer	September 3, 2013	Phase 2
NCT01591421	Canadian Cancer Trials Group\|Pfizer	Metastatic Colorectal Cancer	May 1, 2012	Phase 1\|Phase 2
NCT01540253	Roswell Park Cancer Institute\|Novartis	Unspecified Adult Solid Tumor, Protocol Specific	May 2012	Phase 1
NCT02404844	University Hospital, Essen\|iOMEDICO AG\|Novartis Pharmaceuticals	Breast Cancer	December 2014	Phase 2
NCT01623349	Dana-Farber Cancer Institute\|Novartis\|AstraZeneca	Ovarian Cancer\|Breast Cancer	September 2012	Phase 1
NCT04338399	Adlai Nortye Biopharma Co., Ltd.	Head and Neck Cancer	December 12, 2020	Phase 3
NCT01723800	City of Hope Medical Center\|National Cancer Institute (NCI)	Recurrent Non-small Cell Lung Cancer\|Stage IV Non-small Cell Lung Cancer	July 2013	Phase 1
NCT02117817	Rutgers, The State University of New Jersey\|Rutgers Cancer Institute of New Jersey\|National Cancer Institute (NCI)	Ovarian Cancer\|Endometrial Cancer\|Recurrent Ovarian Cancer\|Recurrent Endometrial Cancer	February 2015	Phase 1
NCT01473901	Novartis Pharmaceuticals\|Novartis	Glioblastoma	December 30, 2011	Phase 1
NCT01501604	Massachusetts General Hospital\|Novartis Pharmaceuticals	Lung Cancer\|Breast Cancer\|Colorectal Cancer\|Cholangiocarcinoma\|Solid Tumors	January 2012	Phase 2
NCT01283503	Novartis Pharmaceuticals\|Novartis	Advanced Solid Tumor	October 2009	Phase 1
NCT01790932	Dana-Farber Cancer Institute	Breast Cancer	June 2012	Phase 2
NCT01283048	Toni Choueiri, MD\|Beth Israel Deaconess Medical Center\|Dana-Farber Cancer Institute	Renal Cell Carcinoma	September 2011	Phase 1
NCT01830504	Hospices Civils de Lyon	Thyroid Cancers	April 2013	Phase 2
NCT02154776	Novartis Pharmaceuticals\|Novartis	Advanced or Metastatic Breast Cancer	June 27, 2014	Phase 1
NCT01304602	University of Kansas Medical Center	Colorectal Cancer	February 2011	Phase 1
NCT01132664	Novartis Pharmaceuticals\|Novartis	Metastatic Breast Cancer\|HER2&addition; Breast Cancer	May 2010	Phase 1\|Phase 2
NCT01550380	University of Utah\|Novartis	Endometrial Cancer	May 2014	Phase 2
NCT01870726	Novartis Pharmaceuticals\|Novartis	c-MET Inhibitor; PI3K Inhibitor, PTEN Mutations, Homozygous Del. of PTEN or PTEN Neg. by IHC, c-Met Ampli. by FISH, INC280, BKM120, Buparlisib; Recurrent GBM	January 9, 2014	Phase 1\|Phase 2
NCT01633060	Novartis Pharmaceuticals\|Novartis	Metastatic Breast Cancer	October 3, 2012	Phase 3
NCT01576666	Novartis Pharmaceuticals\|Novartis	Dose Escalation\|Safety\|Preliminary Efficacy\|Advanced Solid Tumors\|Metastatic Breast Cancer\|Advanced Pancreatic Adenocarcinoma\|Metastatic Colorectal Cancer\|Recurrent Glioblastoma Multiforme\|Gastric Cancer\|Gastroesophageal Junction Cancer\|Triple Negative Metastatic Breast Cancer\|Hormone Receptor Positive (ER&addition;+PR&addition;, and Her2-) Metastatic Breast Cancer	July 2012	Phase 1
NCT01852292	Novartis Pharmaceuticals\|Novartis	Head and Neck Squamous Cell Carcinoma	October 1, 2013	Phase 2
NCT01297452	Memorial Sloan Kettering Cancer Center\|Novartis Pharmaceuticals\|Sai Life Sciences	Solid Tumors	February 15, 2011	Phase 1
NCT01923168	Novartis Pharmaceuticals\|Novartis	Breast Cancer	March 11, 2014	Phase 2
NCT02048787	Novartis Pharmaceuticals\|Novartis	Renal Impairment	March 2014	Phase 1
NCT01248494	Vanderbilt-Ingram Cancer Center	Metastatic Breast Cancer	November 2010	Phase 1
NCT01571024	UNC Lineberger Comprehensive Cancer Center	Advanced Solid Tumors\|Metastatic Colorectal Cancer\|Metastatic Pancreatic Cancer	May 2012	Phase 1
NCT02487823	Institut Paoli-Calmettes\|Novartis	Non Castrate Metastatic Prostate Cancer	October 2014	Phase 1
NCT01570296	National Cancer Centre, Singapore\|Novartis	Non-Small Cell Lung Cancer\|Solid Tumors	October 3, 2011	Phase 1
NCT01833169	Novartis Pharmaceuticals\|Novartis	PI3K Pathway Activated Tumors	March 29, 2013	Phase 2
NCT02303041	Anne Chang\|Novartis Pharmaceuticals\|Stanford University	Carcinoma, Basal Cell\|Recurrent Skin Cancer\|Skin Neoplasms\|Basal Cell Nevus Syndrome	February 2015	Phase 2
NCT01470209	Emory University\|Novartis Pharmaceuticals	Solid Tumors\|Lung Cancer	January 2012	Phase 1
NCT02035124	SCRI Development Innovations, LLC\|Novartis	Advanced Prostate Cancer	April 2014	Phase 2
NCT02058381	Novartis Pharmaceuticals\|Novartis	Pre-menopausal Breast Cancer\|PI3K Pathway Inhibition	May 6, 2014	Phase 1
NCT01934361	Novartis Pharmaceuticals\|Novartis	Recurrent Glioblastoma Multiforme	February 28, 2014	Phase 1
NCT01397877	ARCAGY+ GINECO GROUP	Endometrial Cancer	December 2011	Phase 2
NCT01806649	Prince of Songkla University	Esophageal Cancer	July 1, 2013	Phase 2
NCT01971489	Roswell Park Cancer Institute\|National Cancer Institute (NCI)	Adult Solid Neoplasm\|Recurrent Non-Small Cell Lung Carcinoma\|Stage IIIA Non-Small Cell Lung Cancer\|Stage IIIB Non-Small Cell Lung Cancer\|Stage IV Non-Small Cell Lung Cancer	September 2015	Phase 1
NCT02220855	Patrick Joseph Loehrer Sr.\|Novartis Pharmaceuticals\|Indiana University	Thymoma	October 1, 2014	Phase 2
NCT01730248	Novartis Pharmaceuticals\|Incyte Corporation\|Novartis	Myelofibrosis	December 18, 2012	Phase 1
NCT01487265	SCRI Development Innovations, LLC\|Novartis	Non Small Cell Lung Cancer	March 2014	Phase 2
NCT02452294	University Hospital Tuebingen\|University Hospital Dresden	Malignant Melanoma\|Metastases	July 2015	Phase 2
NCT01468688	Novartis Pharmaceuticals\|Novartis	3rd Line GIST	April 20, 2012	Phase 1
NCT01513356	Sofia Perea, Director Clinical Trials Unit.\|Novartis\|Grupo Hospital de Madrid	Breast Cancer	October 2012	Early Phase 1
NCT01741753	Dana-Farber Cancer Institute	Prostate Cancer	November 2012	Phase 1
NCT01385293	Andrew J. Armstrong, MD\|Novartis Pharmaceuticals\|Duke University	Prostate Cancer\|Metastatic (Spread to Other Areas of the Body)	August 2011	Phase 2
NCT02000882	US Oncology Research\|Novartis Pharmaceuticals	Brain Metastases\|Breast Cancer\|Metastatic Breast Cancer	May 29, 2014	Phase 2
NCT01695473	Won Kim\|Novartis\|University of California, San Francisco	High Risk Prostate Cancer	April 23, 2013	Phase 2
NCT01613677	Novartis Pharmaceuticals\|Novartis	Treatment for Metastatic or Locally Advanced Cervical Cancer	November 2015	Phase 2
NCT02128724	University of Oxford\|Cancer Research UK\|Novartis	Carcinoma, Non-Small-Cell Lung	April 2013	Phase 1
NCT01068483	Novartis Pharmaceuticals\|Novartis	Breast Cancer\|Colon Cancer\|Ovarian Cancer\|Endometrium Cancer	November 2008	Phase 1
NCT02194049	University of California, Davis\|Novartis	Extensive Stage Small Cell Lung Cancer\|Unspecified Adult Solid Tumor, Protocol Specific	July 2014	Phase 1
NCT02301364	Memorial Sloan Kettering Cancer Center\|Novartis	Lymphoma\|Primary Central Nervous System Lymphoma\|Recurrent+Refractory Secondary Central Nervous System Lymphoma	November 20, 2014	Phase 2
NCT01551030	Memorial Sloan Kettering Cancer Center\|Novartis	Metastatic Transitional Cell Carcinoma of the Urothelium	March 2012	Phase 2
NCT01339052	Patrick Y. Wen, MD\|Brigham and Women´s Hospital\|Massachusetts General Hospital\|Novartis Pharmaceuticals\|M.D. Anderson Cancer Center\|Memorial Sloan Kettering Cancer Center\|University of California, San Francisco\|University of California, Los Angeles\|University of Utah\|Dana-Farber Cancer Institute	Glioblastoma	September 2011	Phase 2
NCT01693614	Novartis Pharmaceuticals\|Novartis	Diffuse Large B-cell Lymphoma, Mantle Cell Lymphoma, Follicular Lymphoma	February 28, 2013	Phase 2
NCT02756247	Memorial Sloan Kettering Cancer Center\|Janssen Scientific Affairs, LLC\|Novartis Pharmaceuticals	Lymphoma\|Mantle Cell Lymphoma\|Follicular Lymphoma\|Diffuse Large B Cell Lymphoma	May 9, 2016	Phase 1
NCT01953445	Washington University School of Medicine	Breast Neoplasms	August 2014	Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : ≥ 50 mg/mL ( 111.89 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2379 mL	11.1894 mL	22.3789 mL
5 mM	0.4476 mL	2.2379 mL	4.4758 mL
10 mM	0.2238 mL	1.1189 mL	2.2379 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (5.59 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (5.59 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (5.59 mM); Clear solution

* All of the co-solvents are available by MCE.