Available from stock

Brigatinib

SKU: B0374

Category: API's & Intermediates

Synonyms: AP26113 , 5-Chloro-N4-[2-(dimethylphosphinyl)phenyl]-N2-[2-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]-2,4-pyrimidinediamine; 1197953-54-0
CAS-Number: C₂₉H₃₉ClN₇O₂P
Molecular Formula: 584.09
Molecular Weight

For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.

Product Data
Handling
Safety Information
Details

Specifications

Purity: ≥98% (HPLC)
Appearance: White to yellow solid
Identity: 1H-NMR

Properties

Solvents: DMSO, ethanol (sligthly), water (insoluble)

Shipping: AMBIENT
Short Term Storage: +4°C
Long Term Storage: -20°C
Handling Advice: Protect from light and moisture.
Use / Stability: Stable for at least 2 years after receipt when stored at -20°C.

Transportation: Not dangerous goods

Description: Brigitanib acts as a tyrosine kinase inhibitor with activity against multiple kinases including ALK, ROS1, insulin-like growth factor 1 receptor and against EGFR deletions and point mutations. It acts by inhibiting ALK phosphorylation and the activation of downstream signaling proteins. It is a highly potent and selective inhibitor of anaplastic lymphoma kinase (ALK). Blocks ALK activity and reduces growth in neuroblastoma cells, mouse xenograft, and Drosophila model systems harboring constitutively active ALK variants. It is potentially useful for the treatment of non-small cell lung cancer (NSCLC). Can be used in combination with anti-EGFR drugs to overcome EGFR mutation resistance.
Smiles: CN1CCN(C2CCN(C3=CC=C(NC4=NC(NC5=CC=CC=C5P(C)(C)=O)=C(Cl)C=N4)C(OC)=C3)CC2)CC1
InChi Key: AILRADAXUVEEIR-UHFFFAOYSA-N
References: (1) R. Katayama, et al., PNAS 108, 7535 (2011) , (2) M. Ceccon, et al., Mol. Cancer Res. 11, 122 (2013) , (3) J.T. Siaw, et al., Oncotarget 7, 29011 (2016) , (4) W.S. Huang, et al., J. Med. Chem. 59, 4948 (2016) , (5) S. Zhang, et al., Clin. Cancer Res. 22, 5527 (2016) , (6) K. Uchibori, et al., Nat. Commun. 8, 14768 (2017) , (7) L. Mezquita & D. Planchard, Cancer Manag. Res. 10, 123 (2018) , (8) S.A. Spencer, et al., Ann. Pharmacother. 53, 621 (2019)

Brigitanib acts as a tyrosine kinase inhibitor with activity against multiple kinases including ALK, ROS1, insulin-like growth factor 1 receptor and against EGFR deletions and point mutations. It acts by inhibiting ALK phosphorylation and the activation of downstream signaling proteins. It is a highly potent and selective inhibitor of anaplastic lymphoma kinase (ALK). Blocks ALK activity and reduces growth in neuroblastoma cells, mouse xenograft, and Drosophila model systems harboring constitutively active ALK variants. It is potentially useful for the treatment of non-small cell lung cancer (NSCLC). Can be used in combination with anti-EGFR drugs to overcome EGFR mutation resistance.

SKU: B0374 Category: API's & Intermediates

Additional information

Additional information

Synonyms	AP26113, 5-Chloro-N4-[2-(dimethylphosphinyl)phenyl]-N2-[2-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]-2,4-pyrimidinediamine
Purity	≥98% (HPLC)
Appearance	White to yellow solid
CAS-Number	1197953-54-0
Molecular Formula	C29H39ClN7O2P
Molecular Weight	584.09
Identity	1H-NMR
Solvents	DMSO, ethanol (sligthly), water (insoluble)
Smiles	CN1CCN(C2CCN(C3=CC=C(NC4=NC(NC5=CC=CC=C5P(C)(C)=O)=C(Cl)C=N4)C(OC)=C3)CC2)CC1
InChi Key	AILRADAXUVEEIR-UHFFFAOYSA-N
Shipping	AMBIENT
Short Term Storage	+4°C
Long Term Storage	-20°C
Handling Advice	Protect from light and moisture.
Use / Stability	Stable for at least 2 years after receipt when stored at -20°C.
Transportation	Not dangerous goods
References	(1) R. Katayama, et al., PNAS 108, 7535 (2011), (2) M. Ceccon, et al., Mol. Cancer Res. 11, 122 (2013), (3) J.T. Siaw, et al., Oncotarget 7, 29011 (2016), (4) W.S. Huang, et al., J. Med. Chem. 59, 4948 (2016), (5) S. Zhang, et al., Clin. Cancer Res. 22, 5527 (2016), (6) K. Uchibori, et al., Nat. Commun. 8, 14768 (2017), (7) L. Mezquita & D. Planchard, Cancer Manag. Res. 10, 123 (2018), (8) S.A. Spencer, et al., Ann. Pharmacother. 53, 621 (2019)
Quantity	5 mg, Bulk