Amuvatinib (MP-470)
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 201950

CAS#: 850879-09-3

Description: Amuvatinib, also known as MP-470, is an orally bioavailable synthetic carbothioamide with potential antineoplastic activity. Multitargeted receptor tyrosine kinase inhibitor MP470 binds to mutant forms of the stem cell factor receptor (c-Kit; SCFR), inhibiting clinically relevant mutants of this receptor tyrosine kinase that may be associated with resistance to therapy. In addition, MP470 inhibits activities of other receptor tyrosine kinases, such as c-Met, Ret oncoprotein, and mutant forms of Flt3 and PDGFR alpha, which are frequently dysregulated in variety of tumors.


Price and Availability

Size
Price

10mg
USD 90
100mg
USD 450
1g
USD 1950
Size
Price

25mg
USD 150
200mg
USD 750
2g
USD 2950
Size
Price

50mg
USD 250
500mg
USD 1250
5g
Ask price

Amuvatinib (MP470), 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.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 201950
Name: Amuvatinib (MP-470)
CAS#: 850879-09-3
Chemical Formula: C23H21N5O3S
Exact Mass: 447.13651
Molecular Weight: 447.51
Elemental Analysis: C, 61.73; H, 4.73; N, 15.65; O, 10.73; S, 7.17


Synonym: MP470; Amuvatinib; HPK 56; HPK-56; HPK56; MP470; MP-470; MP 470

IUPAC/Chemical Name: N-(benzo[d][1,3]dioxol-5-ylmethyl)-4-(benzofuro[3,2-d]pyrimidin-4-yl)piperazine-1-carbothioamide.

InChi Key: FOFDIMHVKGYHRU-UHFFFAOYSA-N

InChi Code: InChI=1S/C23H21N5O3S/c32-23(24-12-15-5-6-18-19(11-15)30-14-29-18)28-9-7-27(8-10-28)22-21-20(25-13-26-22)16-3-1-2-4-17(16)31-21/h1-6,11,13H,7-10,12,14H2,(H,24,32)

SMILES Code: S=C(N1CCN(C2=C(OC3=CC=CC=C34)C4=NC=N2)CC1)NCC5=CC=C(OCO6)C6=C5


Technical Data

Appearance:
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).

Harmonized System Code:
293490


Additional Information

According to news published on 15 Apr 2008;  Research data build upon previous results showing that MP-470 exhibits anti-tumor activity in breast and prostate cancer cells. The fact that MP-470 in combination with erlotinib effectively suppressed the HER pathway suggests that concurrent administration of both compounds could represent a new treatment for prostate and breast cancers.
According to news published on
;  Research
 
 
 
 


References

1: Phillip CJ, Zaman S, Shentu S, Balakrishnan K, Zhang J, Baladandayuthapani V, Taverna P, Redkar S, Wang M, Stellrecht CM, Gandhi V. Targeting MET kinase with the small-molecule inhibitor amuvatinib induces cytotoxicity in primary myeloma cells and cell lines. J Hematol Oncol. 2013 Dec 10;6:92. doi: 10.1186/1756-8722-6-92. PubMed PMID: 24326130; PubMed Central PMCID: PMC3878866.

2: Asiedu MK, Beauchamp-Perez FD, Ingle JN, Behrens MD, Radisky DC, Knutson KL. AXL induces epithelial-to-mesenchymal transition and regulates the function of breast cancer stem cells. Oncogene. 2014 Mar 6;33(10):1316-24. doi: 10.1038/onc.2013.57. Epub 2013 Mar 11. PubMed PMID: 23474758; PubMed Central PMCID: PMC3994701.

3: Tibes R, Fine G, Choy G, Redkar S, Taverna P, Oganesian A, Sahai A, Azab M, Tolcher AW. A phase I, first-in-human dose-escalation study of amuvatinib, a multi-targeted tyrosine kinase inhibitor, in patients with advanced solid tumors. Cancer Chemother Pharmacol. 2013 Feb;71(2):463-71. doi: 10.1007/s00280-012-2019-3. Epub 2012 Nov 23. PubMed PMID: 23178951.

4: Gujral TS, Karp RL, Finski A, Chan M, Schwartz PE, MacBeath G, Sorger P. Profiling phospho-signaling networks in breast cancer using reverse-phase protein arrays. Oncogene. 2013 Jul 18;32(29):3470-6. doi: 10.1038/onc.2012.378. Epub 2012 Sep 3. PubMed PMID: 22945653; PubMed Central PMCID: PMC3670968.

5: Choy G, Joshi-Hangal R, Oganesian A, Fine G, Rasmussen S, Collier J, Kissling J, Sahai A, Azab M, Redkar S. Safety, tolerability, and pharmacokinetics of amuvatinib from three phase 1 clinical studies in healthy volunteers. Cancer Chemother Pharmacol. 2012 Jul;70(1):183-90. doi: 10.1007/s00280-012-1821-2. Epub 2012 Feb 15. PubMed PMID: 22349808.

6: Zhao H, Luoto KR, Meng AX, Bristow RG. The receptor tyrosine kinase inhibitor amuvatinib (MP470) sensitizes tumor cells to radio- and chemo-therapies in part by inhibiting homologous recombination. Radiother Oncol. 2011 Oct;101(1):59-65. doi: 10.1016/j.radonc.2011.08.013. Epub 2011 Sep 6. PubMed PMID: 21903282.

7: Baxter PA, Thompson PA, McGuffey LM, Gibson BW, Dauser RC, Nuchtern JG, Shi C, Inloes R, Choy G, Redkar S, Blaney SM. Plasma and cerebrospinal fluid pharmacokinetics of MP470 in non-human primates. Cancer Chemother Pharmacol. 2011 Apr;67(4):809-12. doi: 10.1007/s00280-010-1380-3. Epub 2010 Jun 19. PubMed PMID: 20563581.

8: Welsh JW, Mahadevan D, Ellsworth R, Cooke L, Bearss D, Stea B. The c-Met receptor tyrosine kinase inhibitor MP470 radiosensitizes glioblastoma cells. Radiat Oncol. 2009 Dec 22;4:69. doi: 10.1186/1748-717X-4-69. PubMed PMID: 20028557; PubMed Central PMCID: PMC2806296.

9: Qi W, Cooke LS, Stejskal A, Riley C, Croce KD, Saldanha JW, Bearss D, Mahadevan D. 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 May 11;9:142. doi: 10.1186/1471-2407-9-142. PubMed PMID: 19432987; PubMed Central PMCID: PMC2685437.

10: Mahadevan D, Cooke L, Riley C, Swart R, Simons B, Della Croce K, Wisner L, Iorio M, Shakalya K, Garewal H, Nagle R, Bearss D. A novel tyrosine kinase switch is a mechanism of imatinib resistance in gastrointestinal stromal tumors. Oncogene. 2007 Jun 7;26(27):3909-19. Epub 2007 Feb 26. PubMed PMID: 17325667.