Lapatinib Ditosylate - CAS 388082-77-7
Catalog number: 388082-77-7
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C29H26ClFN4O4S.2C7H8O3S
Molecular Weight:
925.46
COA:
Inquire
Targets:
EGFR
Description:
Lapatinib is a synthetic, orally-active quinazoline with potential antineoplastic activity. Lapatinib reversibly blocks phosphorylation of the epidermal growth factor receptor (EGFR), ErbB2, and the Erk-1 and-2 and AKT kinases; it also inhibits cyclin D protein levels in human tumor cell lines and xenografts. EGFR and ErbB2 have been implicated in the growth of various tumor types.
Publictions citing BOC Sciences Products
  • >> More
Purity:
>98%
Synonyms:
GW-572016
MSDS:
Inquire
1.Neratinib Plus Paclitaxel vs Trastuzumab Plus Paclitaxel in Previously Untreated Metastatic ERBB2-Positive Breast Cancer: The NEfERT-T Randomized Clinical Trial.
Awada A1, Colomer R2, Inoue K3, Bondarenko I4, Badwe RA5, Demetriou G6, Lee SC7, Mehta AO8, Kim SB9, Bachelot T10, Goswami C11, Deo S12, Bose R13, Wong A14, Xu F14, Yao B14, Bryce R14, Carey LA15. JAMA Oncol. 2016 Apr 14. doi: 10.1001/jamaoncol.2016.0237. [Epub ahead of print]
Importance: Efficacious ERBB2 (formerly HER2 or HER2/neu)-directed treatments, in addition to trastuzumab and lapatinib, are needed.
2.Characterization of the binding of an anticancer drug, lapatinib to human serum albumin.
Kabir MZ1, Mukarram AK2, Mohamad SB3, Alias Z1, Tayyab S4. J Photochem Photobiol B. 2016 Apr 13;160:229-239. doi: 10.1016/j.jphotobiol.2016.04.005. [Epub ahead of print]
Interaction of a promising anticancer drug, lapatinib (LAP) with the major transport protein in human blood circulation, human serum albumin (HSA) was investigated using fluorescence and circular dichroism (CD) spectroscopy as well as molecular docking analysis. LAP-HSA complex formation was evident from the involvement of static quenching mechanism, as revealed by the fluorescence quenching data analysis. The binding constant, Ka value in the range of 1.49-1.01×105M-1, obtained at three different temperatures was suggestive of the intermediate binding affinity between LAP and HSA. Thermodynamic analysis of the binding data (∆H=-9.75kJmol-1 and ∆S=+65.21Jmol-1K-1) suggested involvement of both hydrophobic interactions and hydrogen bonding in LAP-HSA interaction, which were in line with the molecular docking results. LAP binding to HSA led to the secondary and the tertiary structural alterations in the protein as evident from the far-UV and the near-UV CD spectral analysis, respectively.
3.Ridaforolimus improves the anti-tumor activity of dual HER2 blockade in uterine serous carcinoma in vivo models with HER2 gene amplification and PIK3CA mutation.
Hernandez SF1, Chisholm S2, Borger D3, Foster R4, Rueda BR4, Growdon WB5. Gynecol Oncol. 2016 Apr 1. pii: S0090-8258(16)30083-X. doi: 10.1016/j.ygyno.2016.03.027. [Epub ahead of print]
OBJECTIVE: Uterine serous carcinomas (USC) harbor simultaneous HER2 (ERBB2) over-expression and gain of function mutations in PIK3CA. These concurrent alterations may uncouple single agent anti-HER2 therapeutic efficacy making inhibition of the mammalian target of rapamycin (mTOR) a promising option to heighten anti-tumor response.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related EGFR Products


NRC-2694
(CAS: 936446-61-6)

NRC-2694 is a small molecule antagonist of epidermal growth factor receptor (EGFR) signalling pathways, for the treatment of solid tumors.

CAS 211555-04-3 WHI-P154

WHI-P154
(CAS: 211555-04-3)

WHI-P154 is a JAK3 inhibitor with IC50 = 1.8 μM. WHI-P154 displays no activity at JAK1 or JAK2. WHI-P154 also Inhibits STAT1 activation, iNOS expression and N...

Epertinib
(CAS: 908305-13-5)

Epertinib, also known as S-222611, is a potent, oral, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with IC50s of 1.48 nM, 7.15 nM...

Pyrotinib
(CAS: 1269662-73-8)

Pyrotinib, also known as SHR-1258, is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively. Upon oral administration, pyroti...

CAS 1204313-51-8 Icotinib Hydrochloride

Icotinib Hydrochloride
(CAS: 1204313-51-8)

Icotinib Hydrochloride is a quinazoline-based inhibitor of epidermal growth factor receptor (EGFR), which is upregulated in a variety of cancer cell types. Icot...

ZD-4190
(CAS: 413599-62-9)

ZD-4190, a substituted 4-anilinoquinazoline, is a potent, orally available inhibitor of the vascular endothelial cell growth factor receptor 2 (VEGFR2) and of e...

NT113
(CAS: 1398833-56-1)

NT113 is a pan-ERBB inhibitor with high brain penetrance. It can inhibit the growth of glioblastoma xenografts with EGFR amplification. NT113 is active against ...

CAS 231277-92-2 Lapatinib

Lapatinib
(CAS: 231277-92-2)

Lapatinib, used in the form of Lapatinib Ditosylate, is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM, respectively.

CAS 1213269-23-8 WZ-4002

WZ-4002
(CAS: 1213269-23-8)

Transtinib
(CAS: 1246089-27-9)

This active molecular is an irreversible EGFR ( epidermal growth factor receptor ) tyrosine kinase inhibitor. Transtinib shows good anti-proliferative activity ...

CAS 1173023-85-2 GW 583340 dihydrochloride

GW 583340 dihydrochloride
(CAS: 1173023-85-2)

GW 583340 dihydrochloride is a potent dual EGFR/ErbB2 tyrosine kinase inhibitor (IC50 = 0.01 and 0.014 μM, respectively). GW 583340 selectively inhibits growth ...

CAS 873837-23-1 BMS-599626 Hydrochloride

BMS-599626 Hydrochloride
(CAS: 873837-23-1)

BMS-599626 Hydrochloride is a selective and efficacious orally bioavailable inhibitor of the HER1, HER2 and HER4 tyrosine kinases with potential antineoplastic ...

BMS 599626 dihydrochloride

BMS 599626 dihydrochloride is a potent and selective EGFR and ErbB2 inhibitor (IC50 = 22 nM and 32 nM, respectively), and also inhibits HER4 (IC50 = 190 nM). BM...

Trastuzumab
(CAS: 180288-69-1)

Trastuzumab is a monoclonal antibody drug for the treatment of breast cancer which is HER2 receptor positive. It acts via binding to HER2 receptor to suppress c...

CAS 133550-30-8 AG-490

AG-490
(CAS: 133550-30-8)

Tyrphostin AG490 is a JAK-2 specific inhibitor, which inhibits phosphorylation of EGFR and signal transducer and activator of transcription 3 [STAT-3], and subs...

CAS 1110813-31-4 Dacomitinib

Dacomitinib
(CAS: 1110813-31-4)

Dacomitinib, aslo known as PF-299 and PF-00299804; or PF299804, is an orally bioavailable, highly selective, second-generation small-molecule inhibitor of the p...

CAS 184475-35-2 Gefitinib

Gefitinib
(CAS: 184475-35-2)

Gefitinib effectively inhibits all tyrosine phosphorylation sites on EGFR in both the high and low-EGFR-expressing cell lines including NR6, NR6M and NR6W cell ...

CAS 383432-38-0 CP-724714

CP-724714
(CAS: 383432-38-0)

CP-724714 is An orally bioavailable quinazoline with potential antineoplastic activity. CP-724,714 selectively binds to the intracellular domain of HER2, revers...

CAS 451493-31-5 AV-412 Tosylate

AV-412 Tosylate
(CAS: 451493-31-5)

AV-412 is a dual EGFR/ErbB2 kinase inhibitor. It completely inhibits the tumor growth of both H1650 and H1975 xenografts in nude mice. It is proved that AV-412 ...

CAS 781613-23-8 XL-647

XL-647
(CAS: 781613-23-8)

XL647 is an orally bioavailable small-molecule receptor tyrosine kinase inhibitor with potential antineoplastic activity. It inhibits EGFR, HER2, VEGFR and EphB...

Chemical Structure

CAS 388082-77-7 Lapatinib Ditosylate

Quick Inquiry

Verification code

Featured Items