Amuvatinib
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Hodoodo CAT#: H201950

CAS#: 850879-09-3 (free)

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.


Chemical Structure

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Amuvatinib
CAS# 850879-09-3 (free)

Theoretical Analysis

Hodoodo Cat#: H201950
Name: Amuvatinib
CAS#: 850879-09-3 (free)
Chemical Formula: C23H21N5O3S
Exact Mass: 447.14
Molecular Weight: 447.510
Elemental Analysis: C, 61.73; H, 4.73; N, 15.65; O, 10.73; S, 7.17

Price and Availability

Size Price Availability Quantity
25mg USD 160 2 Weeks
50mg USD 310 2 Weeks
100mg USD 540 2 Weeks
200mg USD 970 2 Weeks
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Related CAS #: 850879-09-3 (free); 1055986-67-8 (hydrochloride)  

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

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

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).

HS Tariff Code: 2934.99.9001

More Info: 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        

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 447.51 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.

Recalculate based on batch purity %
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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Marciano R, David HB, Akabayov B, Rotblat B. The Amuvatinib Derivative, N-(2H -1,3-Benzodioxol-5-yl)-4-{thieno[3,2-d]pyrimidin-4-yl}piperazine-1-carboxamide, Inhibits Mitochondria and Kills Tumor Cells under Glucose Starvation. Int J Mol Sci. 2020 Feb 4;21(3):1041. doi: 10.3390/ijms21031041. PMID: 32033217; PMCID: PMC7036964.


2: Huynh TTX, Pham TX, Lee GH, Lee JB, Lee SG, Tark D, Lim YS, Hwang SB. Amuvatinib Blocks SARS-CoV-2 Infection at the Entry Step of the Viral Life Cycle. Microbiol Spectr. 2023 Mar 30:e0510522. doi: 10.1128/spectrum.05105-22. Epub ahead of print. PMID: 36995225.


3: Fedorenko IV, Fang B, Koomen JM, Gibney GT, Smalley KS. Amuvatinib has cytotoxic effects against NRAS-mutant melanoma but not BRAF-mutant melanoma. Melanoma Res. 2014 Oct;24(5):448-53. doi: 10.1097/CMR.0000000000000103. PMID: 24950457; PMCID: PMC4384823.


4: Chang JY, Verma V, Welsh JW, Formenti SC. Radiotherapy plus immune checkpoint blockade in PD(L)-1-resistant metastatic NSCLC. Lancet Oncol. 2022 Apr;23(4):e156. doi: 10.1016/S1470-2045(22)00134-6. PMID: 35358456.


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. PMID: 22349808.


6: Chen D, Barsoumian HB, Yang L, Younes AI, Verma V, Hu Y, Menon H, Wasley M, Masropour F, Mosaffa S, Ozgen T, Klein K, Cortez MA, Welsh JW. SHP-2 and PD-L1 Inhibition Combined with Radiotherapy Enhances Systemic Antitumor Effects in an Anti-PD-1-Resistant Model of Non-Small Cell Lung Cancer. Cancer Immunol Res. 2020 Jul;8(7):883-894. doi: 10.1158/2326-6066.CIR-19-0744. Epub 2020 Apr 16. PMID: 32299915; PMCID: PMC10173258.


7: Chen D, Barsoumian HB, Fischer G, Yang L, Verma V, Younes AI, Hu Y, Masropour F, Klein K, Vellano C, Marszalek J, Davies M, Cortez MA, Welsh J. Combination treatment with radiotherapy and a novel oxidative phosphorylation inhibitor overcomes PD-1 resistance and enhances antitumor immunity. J Immunother Cancer. 2020 Jun;8(1):e000289. doi: 10.1136/jitc-2019-000289. PMID: 32581056; PMCID: PMC7319777.


8: Mita M, Gordon M, Rosen L, Kapoor N, Choy G, Redkar S, Taverna P, Oganesian A, Sahai A, Azab M, Bristow R, Tolcher AW. Phase 1B study of amuvatinib in combination with five standard cancer therapies in adults with advanced solid tumors. Cancer Chemother Pharmacol. 2014 Jul;74(1):195-204. doi: 10.1007/s00280-014-2481-1. Epub 2014 May 22. PMID: 24849582.


9: 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. PMID: 21903282.


10: Byers LA, Horn L, Ghandi J, Kloecker G, Owonikoko T, Waqar SN, Krzakowski M, Cardnell RJ, Fujimoto J, Taverna P, Azab M, Camidge DR. A phase 2, open-label, multi-center study of amuvatinib in combination with platinum etoposide chemotherapy in platinum-refractory small cell lung cancer patients. Oncotarget. 2017 Aug 3;8(46):81441-81454. doi: 10.18632/oncotarget.19888. PMID: 29113403; PMCID: PMC5655298.


11: 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. PMID: 23178951.


12: 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. Erratum in: J Hematol Oncol. 2016 Oct 13;9(1):110. PMID: 24326130; PMCID: PMC3878866.


13: Brayford S, Duly A, Teo WS, Dwarte T, Gonzales-Aloy E, Ma Z, McVeigh L, Failes TW, Arndt GM, McCarroll JA, Kavallaris M. βIII-tubulin suppression enhances the activity of Amuvatinib to inhibit cell proliferation in c-Met positive non-small cell lung cancer cells. Cancer Med. 2023 Feb;12(4):4455-4471. doi: 10.1002/cam4.5128. Epub 2022 Aug 10. PMID: 35946957; PMCID: PMC9972117.


14: Phillip CJ, Zaman S, Shentu S, Balakrishnan K, Zhang J, Baladandayuthapani V, Taverna P, Redkar S, Wang M, Stellrecht CM, Gandhi V. Erratum to: Targeting MET kinase with the small-molecule inhibitor amuvatinib induces cytotoxicity in primary myeloma cells and cell lines. J Hematol Oncol. 2016 Oct 13;9(1):110. doi: 10.1186/s13045-016-0335-5. Erratum for: J Hematol Oncol. 2013 Dec 10;6:92. PMID: 27737688; PMCID: PMC5064904.


15: Padda S, Neal JW, Wakelee HA. MET inhibitors in combination with other therapies in non-small cell lung cancer. Transl Lung Cancer Res. 2012 Dec;1(4):238-53. doi: 10.3978/j.issn.2218-6751.2012.10.08. PMID: 25806189; PMCID: PMC4367550.


16: Son J, Hsieh RC, Lin HY, Krause KJ, Yuan Y, Biter AB, Welsh J, Curran MA, Hong DS. Inhibition of the CD47-SIRPα axis for cancer therapy: A systematic review and meta-analysis of emerging clinical data. Front Immunol. 2022 Nov 11;13:1027235. doi: 10.3389/fimmu.2022.1027235. PMID: 36439116; PMCID: PMC9691650.


17: Salem MSH, Abdel Aziz YM, Elgawish MS, Said MM, Abouzid KAM. Design, synthesis, biological evaluation and molecular modeling study of new thieno[2,3-d]pyrimidines with anti-proliferative activity on pancreatic cancer cell lines. Bioorg Chem. 2020 Jan;94:103472. doi: 10.1016/j.bioorg.2019.103472. Epub 2019 Nov 30. PMID: 31813475.


18: Cortez MA, Masrorpour F, Ivan C, Zhang J, Younes AI, Lu Y, Estecio MR, Barsoumian HB, Menon H, Caetano MDS, Ramapriyan R, Schoenhals JE, Wang X, Skoulidis F, Wasley MD, Calin G, Hwu P, Welsh JW. Bone morphogenetic protein 7 promotes resistance to immunotherapy. Nat Commun. 2020 Sep 24;11(1):4840. doi: 10.1038/s41467-020-18617-z. Erratum in: Nat Commun. 2020 Oct 8;11(1):5144. PMID: 32973129; PMCID: PMC7519103.


19: Sezen D, Barsoumian HB, He K, Hu Y, Wang Q, Abana CO, Puebla-Osorio N, Hsu EY, Wasley M, Masrorpour F, Wang J, Cortez MA, Welsh JW. Pulsed radiotherapy to mitigate high tumor burden and generate immune memory. Front Immunol. 2022 Oct 6;13:984318. doi: 10.3389/fimmu.2022.984318. PMID: 36275767; PMCID: PMC9582356.


20: Nazha B, Owonikoko TK. The clinical conundrum of managing relapsed small cell lung cancer. Cancer. 2019 Apr 1;125(7):1022-1026. doi: 10.1002/cncr.31849. Epub 2018 Dec 18. PMID: 30561759.