MP-470 Inhibitor CAS No. 850879-09-03

Cat. No.	Name	Size	Price
KI0275	MP-470	2 mg	$211.2
	MP-470	5 mg	$369.6
	MP-470	10 mg	$651.2
	MP-470	50 mg	$1531.2

Chemical Characteristic

Product Name	MP-470
Synonyms	Amuvatinib
CAS No.	850879-09-03
Molecular Weight	447.51
Formula	C₂₃H₂₁N₅O₃S
Chemical Name	N-(1,3-benzodioxol-5-ylmethyl)-4-([1]benzofuro[3,2-d]pyrimidin-4-yl)piperazine-1-carbothioamide
Smiles	N1(CCN(CC1)c1c2c(ncn1)c1c(o2)cccc1)C(=S)NCc1cc2OCOc2cc1
Chemical Structure

Biological activities

MP-470 is a novel orally bioavailable mutitargeting tyrosine kinase inhibitor with activity against mutant c-KIT, PDGFRa and FLT3. MP-470 synergizes with docetaxel and is cytotoxic to Gastrointestinal stromal tumors cells (GIST) with IC50 values of 0.3-0.5 µM. ^[1] Meanwhile, MP-470 alone can inhibit eight glioblastoma cells (GBM) with IC50 values ranging from 1 µM to 10 µM (median 5 µM). MP-470 reduces c-Met phosphorylation and enhances radiation-induced cell kill by 0.4 logs in SF767 cells. MP-470 is shown to inhibit dsDNA break repair and increase apoptosis, MP-470 also influences various survival and DNA repair related proteins such as pAKT, RAD51 and GSK3β. The addition of MP-470 to radiation results in a tumor-growth-delay enhancement ratio of 2.9 over radiation alone and extends survival time.^[2] At the same time, MP-470 of 0.66 µM can kill 50% H1299 clonogenic cells, 1-2.5 µM can decrease RAD51 expression with small changes in cell cycle progression in a dose-dependent manner.^[3] Besides that, MP-470 inhibits cell proliferation, induces cell growth arrest and promotes apoptosis in prostate LNCaP and PC-3 cells with IC50s of ~4 µM and 8 mµ. Furthermore, MP-470-Erlotinib combination produces 30-65% dose-dependent tumor growth inhibition in a LNCap mouse xenograft model. ^[4]

Protocols

MP-470 is dissolved in DMSO. ^[2]

References

[1] Mahadevan D, et al. A novel tyrosine kinase switch is a mechanism of imatinib resistance in gastrointestinal stromal tumors. Oncogene. 2007, 26: 3909-3919. [2] James WW, et al. The c-Met receptor tyrosine kinase inhibitor MP-470 radiosensitizes glioblastoma cells. Radiat Oncol. 2009, 4: 69. [3] Helen Z, et al. The receptor tyrosine kinase inhibitor amuvatinib (MP-470) sensitizes tumor cells to radio- and chemo-therapies in part by inhibiting homologous recombination. Radiother Oncol. 2011, 101(1): 59-65. [4] Qi W, e t al. MP470, a novel receptor tyrosine kinase inhibitor,in combination with Erlotinib inhibits the HER family/PI3K/Akt pathway and tumor growth in prostate cancer. BMC Cancer. 2009, 9:142.

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