Avapritinib (BLU-285)

For research use only.

Catalog No.S8553

6 publications

Avapritinib (BLU-285) Chemical Structure

CAS No. 1703793-34-3

Avapritinib (BLU-285) is a small molecule kinase inhibitor that potently inhibits PDGFRα D842V mutant activity in vitro (IC50 = 0.5 nM) and PDGFRα D842V autophosphorylation in the cellular setting (IC50 = 30 nM); also a potent inhibitor of the analogous Kit (c-Kit) mutation, D816V in Kit (c-Kit) Exon 17 (IC50 = 0.5 nM).

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Selleck's Avapritinib (BLU-285) has been cited by 6 publications

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Choose Selective PDGFR Inhibitors

Biological Activity

Description Avapritinib (BLU-285) is a small molecule kinase inhibitor that potently inhibits PDGFRα D842V mutant activity in vitro (IC50 = 0.5 nM) and PDGFRα D842V autophosphorylation in the cellular setting (IC50 = 30 nM); also a potent inhibitor of the analogous Kit (c-Kit) mutation, D816V in Kit (c-Kit) Exon 17 (IC50 = 0.5 nM).
Targets
PDGFRα (D842V) [1]
()
c-Kit (D816V) [1]
()
0.5 nM 0.5 nM
In vitro

BLU-285 is a selective oral inhibitor that targets KIT Exon 17 and PDGFRα D842 activation loop mutants. Cellular assays measuring inhibition of KIT mutant autophosphorylation confirm the activity of BLU-285 against the KIT D816 mutants D816V (HMC1.2 cells, IC50 = 3 nM) and D816Y (P815 cells, IC50 = 22 nM) as well as other KIT Exon 17 mutants such as N822K (Kasumi cells, IC50 = 40 nM) found in treatment-refractory GIST[1].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BA/F3 cells MoHOS5Jwf3SqIHnubIljcXSxbjDhd5NigQ>? NXv1T49kPzJiaB?= NGHGOFRKdmirYnn0bY9vKG:oIFvpeEBFQDF4VjDteZRidnRiKIXub45wf25ib4Lp[4lvMSC2cnHud4Zm[3SnZDDpckBud3W|ZTDCRU9HOyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGxiZ4Lve5RpKGmwY4XiZZRm\CCob4KgO|IhcHK|IHL5JG1VWyCjc4PhfUwhT0l3MDC9JFAvODB6IN88UU4> NYLvNZZkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyNFQ1PDFpPkOwNlA1PDRzPD;hQi=>
BA/F3 cells MXTHdo94fGhiaX7obYJqfG:wIHHzd4F6 NX3lUFNvPzJiaB?= MXzJcohq[mm2aX;uJI9nKFCGR1\SZYxxcGFiVkW2NWQwTDh2Mm[gcZV1[W62IDj1cotvd3ewIH;ybYdqdilidILhcpNn\WO2ZXSgbY4hdW:3c3WgRmEwTjNiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBk\WyuIHfyc5d1cCCrbnP1ZoF1\WRiZn;yJFczKGi{czDifUBOXFNiYYPzZZktKEeLNUCgQUAxNjBzIN88UU4> MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJyNES0NUc,OzB{MES0OFE9N2F-
BA/F3 cells Mnq5S5Jwf3SqIHnubIljcXSxbjDhd5NigQ>? NUj0fItGPzJiaB?= NUDyWFNkUW6qaXLpeIlwdiCxZjDLbZQh\XixbjCxNUBl\WyndHnvckApPTV5IITvJFU2QCC{ZYPp[JVmeyliYX7kJGQ5OT[KIH31eIFvfCBqdX7rco94diCxcnnnbY4qKHS{YX7z[oVkfGWmIHnuJI1wfXOnIFLBM2Y{KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gZ4VtdCCpcn;3eIghcW6ldXLheIVlKG[xcjC3NkBpenNiYomgUXRUKGG|c3H5MEBIUTVyIE2gNE4xOTdizszNMi=> MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJyNES0NUc,OzB{MES0OFE9N2F-
BA/F3 cells M2nQXGdzd3e2aDDpcohq[mm2b36gZZN{[Xl? NFrPN4I4OiCq NFe3e2lKdmirYnn0bY9vKG:oIFvpeEBmgG:wIEGxJIRmdGW2aX;uJEg2PTdidH:gOVU5KHKnc3nkeYV{MSCjbnSgSFgzOEFibYX0ZY51KGGwZDDEPFIxSSCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUB1emGwc3\lZ5Rm\CCrbjDtc5V{\SCEQT;GN{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHPlcIwh\3Kxd4ToJIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IF3UV{Bie3OjeTygS2k2OCB;IECuNFE6KM7:TT6= M{XSO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkC0OFQyLz5|MEKwOFQ1OTxxYU6=
BA/F3 cells NYLwOHM4T3Kxd4ToJIlvcGmkaYTvckBie3OjeR?= MVi3NkBp M{PlRmlvcGmkaYTpc44hd2ZiVFXMMYZ2e2WmIGDES2ZT[mW2YTCoeY5sdm:5bjDvdolocW5rIITyZY5{\mWldHXkJIlvKG2xdYPlJGJCN0Z|IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[2WubDDndo94fGhiaX7jeYJifGWmIH\vdkA4OiCqcoOgZpkhVVSVIHHzd4F6NCCJSUWwJF0hOC5yMkKg{txONg>? MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJyNES0NUc,OzB{MES0OFE9N2F-
BA/F3 cells M3W3S2dzd3e2aDDpcohq[mm2b36gZZN{[Xl? NYXFTGNxPzJiaB?= MVvJcohq[mm2aX;uJI9nKEurdDDlfI9vKDFzIHTlcIV1cW:wIDi1OVchfG9iNUW4JJJme2mmdXXzLUBidmRiQUiyPXAhdXW2YX70JIFv\CC\OEKzSEBufXSjboSgLJVvc26xd36gc5Jq\2mwKTD0doFve2[nY4Tl[EBqdiCvb4Xz[UBDSS:IMzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHyg[5Jwf3SqIHnuZ5Vj[XSnZDDmc5IhPzJiaILzJIJ6KE2WUzDhd5NigSxiR1m1NEA:KDBwMEK4JO69VS5? NEXkeGI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEKwOFQ1OSd-M{CyNFQ1PDF:L3G+
BA/F3 cells NVSwWYlUT3Kxd4ToJIlvcGmkaYTvckBie3OjeR?= MmjBO|IhcA>? NGf0e4RKdmirYnn0bY9vKG:oIFvpeEBXPTZyRD;EPFE3UCCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUB1emGwc3\lZ5Rm\CCrbjDtc5V{\SCEQT;GN{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHPlcIwh\3Kxd4ToJIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IF3UV{Bie3OjeTygS2k2OCB;IECuNFI6KM7:TT6= MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJyNES0NUc,OzB{MES0OFE9N2F-
BA/F3 cells NGnXO2FIem:5dHigbY5pcWKrdH;uJIF{e2G7 NF;VNG04OiCq MkTWTY5pcWKrdHnvckBw\iCWRVyt[pV{\WRiUFTHSnJidHCqYTCoeY5sdm:5bjDvdolocW5rIITyZY5{\mWldHXkJIlvKG2xdYPlJGJCN0Z|IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[2WubDDndo94fGhiaX7jeYJifGWmIH\vdkA4OiCqcoOgZpkhVVSVIHHzd4F6NCCJSUWwJF0hOC5yM{Sg{txONg>? NFXJfXQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEKwOFQ1OSd-M{CyNFQ1PDF:L3G+
BA/F3 cells NYrGWZlET3Kxd4ToJIlvcGmkaYTvckBie3OjeR?= M2jOdVczKGh? MmTaTY5pcWKrdHnvckBw\iCNaYSg[ZhwdiBzMTDk[YxmfGmxbjCoOVU4KHSxIEW1PEBz\XOrZIXld{kh[W6mIF64NlJMKG23dHHueEBidmRiWUiyN2QhdXW2YX70JEh2dmuwb4fuJI9zcWerbjmgeJJidnOoZXP0[YQhcW5ibX;1d4UhSkFxRkOgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJIdzd3e2aDDpcoN2[mG2ZXSg[o9zKDd{IHjyd{BjgSCPVGOgZZN{[XluIFfJOVAhRSByLkCzOEDPxE1w NF\Jbm09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEKwOFQ1OSd-M{CyNFQ1PDF:L3G+
BA/F3 cells M2HmSmdzd3e2aDDpcohq[mm2b36gZZN{[Xl? MkjVO|IhcA>? NIXUZWpKdmirYnn0bY9vKG:oIFvpeEBXPTZyRDDteZRidnRiKIXub45wf25ib4Lp[4lvMSC2cnHud4Zm[3SnZDDpckBud3W|ZTDCRU9HOyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGxiZ4Lve5RpKGmwY4XiZZRm\CCob4KgO|IhcHK|IHL5JG1VWyCjc4PhfUwhT0l3MDC9JFAvODR{IN88UU4> NV2xZ5dsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyNFQ1PDFpPkOwNlA1PDRzPD;hQi=>
BA/F3 cells NEXWTFNIem:5dHigbY5pcWKrdH;uJIF{e2G7 NWLF[FhmPzJiaB?= Ml3LTY5pcWKrdHnvckBw\iCNaYSg[ZhwdiB7IFHZOVAzKHSxIEWwN{BqdnOncoTpc44h[W6mIFS4NVYhdXW2YX70JEh2dmuwb4fuJI9zcWerbjmgeJJidnOoZXP0[YQhcW5ibX;1d4UhSkFxRkOgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJIdzd3e2aDDpcoN2[mG2ZXSg[o9zKDd{IHjyd{BjgSCPVGOgZZN{[XluIFfJOVAhRSByLkC2PUDPxE1w MmLSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{MES0OFEoRjNyMkC0OFQyRC:jPh?=
BA/F3 cells NV3lWWZ7T3Kxd4ToJIlvcGmkaYTvckBie3OjeR?= MUG3NkBp MYXJcohq[mm2aX;uJI9nKEurdDDlfI9vKDFzIHTlcIV1cW:wIDi1OVchfG9iNUW4JJJme2mmdXXzLUBufXSjboSgLJVvc26xd36gc5Jq\2mwKTD0doFve2[nY4Tl[EBqdiCvb4Xz[UBDSS:IMzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHyg[5Jwf3SqIHnuZ5Vj[XSnZDDmc5IhPzJiaILzJIJ6KE2WUzDhd5NigSxiR1m1NEA:KDBwMEe4JO69VS5? NHW5SW49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEKwOFQ1OSd-M{CyNFQ1PDF:L3G+
BA/F3 cells NILGTJhIem:5dHigbY5pcWKrdH;uJIF{e2G7 MofLO|IhcA>? NXXxU4RiUW6qaXLpeIlwdiCxZjDLbZQh\XixbjCxNUBl\WyndHnvckApPTZyIITvJFU4QCC{ZYPp[JVmeylibYX0ZY51KCi3bnvuc5dvKG:{aXfpckkhfHKjboPm[YN1\WRiaX6gcY92e2ViQlGvSlMh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDj[YxtKGe{b4f0bEBqdmO3YnH0[YQh\m:{IEeyJIhzeyCkeTDNWHMh[XO|YYmsJGdKPTBiPTCwMlEyPyEQvF2u NIHqWFM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEKwOFQ1OSd-M{CyNFQ1PDF:L3G+
BA/F3 cells M4TPXWdzd3e2aDDpcohq[mm2b36gZZN{[Xl? M4fDelczKGh? MYDJcohq[mm2aX;uJI9nKEurdDDlfI9vKDliQWm1NFIhfG9iNUCzJIlve2W{dHnvckBufXSjboSgLJVvc26xd36gc5Jq\2mwKTD0doFve2[nY4Tl[EBqdiCvb4Xz[UBDSS:IMzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHyg[5Jwf3SqIHnuZ5Vj[XSnZDDmc5IhPzJiaILzJIJ6KE2WUzDhd5NigSxiR1m1NEA:KDBwMU[3JO69VS5? M2PwUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkC0OFQyLz5|MEKwOFQ1OTxxYU6=
BA/F3 cells M4jTcGdzd3e2aDDpcohq[mm2b36gZZN{[Xl? NWnFNGhIPzJiaB?= MXPJcohq[mm2aX;uJI9nKEurdDDlfI9vKDFzIHTlcIV1cW:wIDi1OVchfG9iNUW4JJJme2mmdXXzLUBidmRiVk[1OGEhdXW2YX70JEh2dmuwb4fuJI9zcWerbjmgeJJidnOoZXP0[YQhcW5ibX;1d4UhSkFxRkOgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJIdzd3e2aDDpcoN2[mG2ZXSg[o9zKDd{IHjyd{BjgSCPVGOgZZN{[XluIFfJOVAhRSByLkK5NkDPxE1w MmTuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{MES0OFEoRjNyMkC0OFQyRC:jPh?=
BA/F3 cells MmjPS5Jwf3SqIHnubIljcXSxbjDhd5NigQ>? MXu3NkBp NWj1WGw1UW6qaXLpeIlwdiCxZjDLbZQhXjV4MFSvWlY2PEFibYX0ZY51KCi3bnvuc5dvKG:{aXfpckkhfHKjboPm[YN1\WRiaX6gcY92e2ViQlGvSlMh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDj[YxtKGe{b4f0bEBqdmO3YnH0[YQh\m:{IEeyJIhzeyCkeTDNWHMh[XO|YYmsJGdKPTBiPTCwMlQzPyEQvF2u M3fK[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkC0OFQyLz5|MEKwOFQ1OTxxYU6=
BA/F3 cells MmX6S5Jwf3SqIHnubIljcXSxbjDhd5NigQ>? M3TlT|czKGh? MVfJcohq[mm2aX;uJI9nKEurdDDlfI9vKDliQWm1NFIhfG9iNUCzJIlve2W{dHnvckBidmRiVk[1OEBufXSjboSgLJVvc26xd36gc5Jq\2mwKTD0doFve2[nY4Tl[EBqdiCvb4Xz[UBDSS:IMzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHyg[5Jwf3SqIHnuZ5Vj[XSnZDDmc5IhPzJiaILzJIJ6KE2WUzDhd5NigSxiR1m1NEA:KDBwN{WxJO69VS5? M3j4ZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkC0OFQyLz5|MEKwOFQ1OTxxYU6=
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... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
PDGFRA / c-KIT / Wee1 / Cdc2 / PARP / γH2AX / CyclinD1 / β-actin; 

PubMed: 33320833     


(C) Immunoblot assays of WCEs from GIST-T1+Cas9 (KIT-dependent) and GIST-T1+D842V KITKO (KIT-independent) cell lines.

33320833
In vivo In vivo, BLU-285 is a well-tolerated, orally bioavailable agent that achieves dose dependent tumor growth inhibition in a D816Y-driven xenograft model. A PK-PD-efficacy relationship with BLU-285 has been established demonstrating that tumor regression results from >90% target suppression and is observed with 30 mg/kg once daily dosing. With potent activity against PDGFRα D842V and KIT Exon 17 mutants, BLU-285 targets previously unaddressed genomic drivers of disease and provides promise for the treatment of PDGFRα D842V-driven GIST(gastrointestinal stromal tumor) or SM(systemic mastocytosis), where more than 90% of patients carry the KIT D816V mutation. Besides single agent activity, the highly selective BLU-285 offers an opportunity for combination with other agents in GIST to cover the entirety of KIT primary and resistance mutants[1].

Protocol

Animal Research:

[1]

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  • Animal Models: mice
  • Dosages: 10 or 30 mg/kg
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 66 mg/mL (132.38 mM)
Water Insoluble
Ethanol '''''3 mg/mL
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+40% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.
4mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 498.56
Formula

C26H27FN10

CAS No. 1703793-34-3
Storage powder
in solvent
Synonyms N/A
Smiles CC(C1=CC=C(C=C1)F)(C2=CN=C(N=C2)N3CCN(CC3)C4=NC=NN5C4=CC(=C5)C6=CN(N=C6)C)N

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Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04695431 Enrolling by invitation -- Advanced Systemic Mastocytosis|Aggressive Systemic Mastocytosis|Systemic Mastocytosis With an Associated Hematological Neoplasm|Mast Cell Leukemia Blueprint Medicines Corporation|Analysis Group Inc. December 2 2020 --
NCT03731260 Recruiting Drug: Avapritinib|Drug: Placebo Indolent Systemic Mastocytosis Blueprint Medicines Corporation April 16 2019 Phase 2
NCT03580655 Active not recruiting Drug: Avapritinib Advanced Systemic Mastocytosis|Aggressive Systemic Mastocytosis|Systemic Mastocytosis With an Associated Hematologic Neoplasm|Mast Cell Leukemia Blueprint Medicines Corporation November 21 2018 Phase 2
NCT03465722 Active not recruiting Drug: avapritinib|Drug: regorafenib GIST Blueprint Medicines Corporation March 26 2018 Phase 3
NCT02561988 Active not recruiting Drug: Avapritinib Aggressive Systemic Mastocytosis|Systemic Mastocytosis-associated Hematologic Non-mast Cell Disease|Mast Cell Leukemia|Relapsed or Refractory Myeloid Malignancies Blueprint Medicines Corporation March 10 2016 Phase 1
NCT02508532 Active not recruiting Drug: Avapritinib Gastrointestinal Stromal Tumors (GIST)|Other Relapsed or Refractory Solid Tumors Blueprint Medicines Corporation August 2015 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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PDGFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID