Mubritinib
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MedKoo CAT#: 206800

CAS#: 366017-09-6

Description: Mubritinib, also known as TAK-165, is a protein kinase inhibitor which was under development by Takeda for the treatment of cancer. It completed phase I clinical trials (may be discontinued since 2008). Mubritinib(TAK 165) is a potent EGFR, HER2 and p34cdc2 inhibitor with IC50 of 6 nM and 0.2 µM, respectively. Mubritinib(TAK 165) also inhibits p33cdk2 and p33cdk5. Mubritinib(TAK 165) displays > 4000-fold selectivity over EGFR, FGFR, PDGFR, JAK1 and Src. Mubritinib(TAK 165) exhibits potent antiproliferative effects in ErbB2-overexpressing cancer cell lines (IC50 = 5 nM in BT474 breast cancer cells) and significantly inhibits bladder, breast and prostate cancer xenograft growth in vivo. (source: http://en.wikipedia.org/wiki/Mubritinib).


Chemical Structure

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Mubritinib
CAS# 366017-09-6

Theoretical Analysis

MedKoo Cat#: 206800
Name: Mubritinib
CAS#: 366017-09-6
Chemical Formula: C25H23F3N4O2
Exact Mass: 468.17731
Molecular Weight: 468.47093
Elemental Analysis: C, 64.10; H, 4.95; F, 12.17; N, 11.96; O, 6.83

Size Price Shipping out time Quantity
50mg USD 250 2 Weeks
100mg USD 450 2 Weeks
200mg USD 750 2 Weeks
500mg USD 1650 2 Weeks
1g USD 2750 2 Weeks
2g USD 4950 2 Weeks
5g USD 6950 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2021-03-06. Prices are subject to change without notice.

Mubritinib (TAK-165), purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.

Synonym: Mubritinib; TAK 165; TAK-165; TAK165

IUPAC/Chemical Name: (E)-4-((4-(4-(1H-1,2,3-triazol-1-yl)butyl)phenoxy)methyl)-2-(4-(trifluoromethyl)styryl)oxazole

InChi Key: ZTFBIUXIQYRUNT-MDWZMJQESA-N

InChi Code: InChI=1S/C25H23F3N4O2/c26-25(27,28)21-9-4-20(5-10-21)8-13-24-30-22(18-34-24)17-33-23-11-6-19(7-12-23)3-1-2-15-32-16-14-29-31-32/h4-14,16,18H,1-3,15,17H2/b13-8+

SMILES Code: FC(C1=CC=C(C=C1)/C=C/C2=NC(COC3=CC=C(CCCCN4N=NC=C4)C=C3)=CO2)(F)F

Appearance:
white solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001

Handling Instructions:

Preparing Stock Solutions

The following data is based on the product molecular weight 468.47093 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1. Hayashi, K.; Masuda, S.; Kimura, H. Impact of biomarker usage on oncology drug development. Journal of Clinical Pharmacy and Therapeutics (2013), 38(1), 62-67.

2. Anastassiadis, Theonie; Deacon, Sean W.; Devarajan, Karthik; Ma, Haiching; Peterson, Jeffrey R.Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nature Biotechnology (2011), 29(11), 1039-1045.

3. Grinshtein, Natalie; Datti, Alessandro; Fujitani, Mayumi; Uehling, David; Prakesch, Michael; Isaac, Methvin; Irwin, Meredith S.; Wrana, Jeffrey L.; Al-Awar, Rima; Kaplan, David R. Small Molecule Kinase Inhibitor Screen Identifies Polo-Like Kinase 1 as a Target for Neuroblastoma Tumor-Initiating Cells. Cancer Research (2011), 71(4), 1385-1395.

4. Nagasawa, Joji; Mizokami, Atsushi; Koshida, Kiyoshi; Yoshida, Sei; Naito, Kenichiro; Namiki, Mikio. Novel HER2 selective tyrosine kinase inhibitor, TAK-165, inhibits bladder, kidney and androgen-independent prostate cancer in vitro and in vivo. International Journal of Urology (2006), 13(5), 587-592.

5. Sugita, Shozo; Kawashima, Hidenori; Tanaka, Tomoaki; Kurisu, Takeshi; Sugimura, Kazunobu; Nakatani, Tatsuya Effect of type I growth factor receptor tyrosine kinase inhibitors on phosphorylation and transactivation activity of the androgen receptor in prostate cancer cells: Ligand-independent activation of the N-terminal domain of the androgen receptor. Oncology Reports (2004), 11(6), 1273-1279.



Additional Information