<?xml version="1.0"?>
<ownershipDocument>

    <schemaVersion>X0306</schemaVersion>

    <documentType>4</documentType>

    <periodOfReport>2017-09-19</periodOfReport>

    <issuer>
        <issuerCik>0001069308</issuerCik>
        <issuerName>Acer Therapeutics Inc.</issuerName>
        <issuerTradingSymbol>ACER</issuerTradingSymbol>
    </issuer>

    <reportingOwner>
        <reportingOwnerId>
            <rptOwnerCik>0001717241</rptOwnerCik>
            <rptOwnerName>Schelling Chris</rptOwnerName>
        </reportingOwnerId>
        <reportingOwnerAddress>
            <rptOwnerStreet1>222 THIRD STREET</rptOwnerStreet1>
            <rptOwnerStreet2>SUITE #2240</rptOwnerStreet2>
            <rptOwnerCity>CAMBRIDGE</rptOwnerCity>
            <rptOwnerState>MA</rptOwnerState>
            <rptOwnerZipCode>02142</rptOwnerZipCode>
            <rptOwnerStateDescription></rptOwnerStateDescription>
        </reportingOwnerAddress>
        <reportingOwnerRelationship>
            <isDirector>true</isDirector>
            <isOfficer>true</isOfficer>
            <officerTitle>President and CEO</officerTitle>
        </reportingOwnerRelationship>
    </reportingOwner>

    <nonDerivativeTable>
        <nonDerivativeTransaction>
            <securityTitle>
                <value>Common Stock</value>
            </securityTitle>
            <transactionDate>
                <value>2017-09-19</value>
            </transactionDate>
            <transactionCoding>
                <transactionFormType>4</transactionFormType>
                <transactionCode>J</transactionCode>
                <equitySwapInvolved>false</equitySwapInvolved>
                <footnoteId id="F1"/>
            </transactionCoding>
            <transactionAmounts>
                <transactionShares>
                    <value>1750000</value>
                </transactionShares>
                <transactionPricePerShare>
                    <footnoteId id="F1"/>
                </transactionPricePerShare>
                <transactionAcquiredDisposedCode>
                    <value>A</value>
                </transactionAcquiredDisposedCode>
            </transactionAmounts>
            <postTransactionAmounts>
                <sharesOwnedFollowingTransaction>
                    <value>1750000</value>
                </sharesOwnedFollowingTransaction>
            </postTransactionAmounts>
            <ownershipNature>
                <directOrIndirectOwnership>
                    <value>D</value>
                </directOrIndirectOwnership>
            </ownershipNature>
        </nonDerivativeTransaction>
    </nonDerivativeTable>

    <footnotes>
        <footnote id="F1">Received in connection with the Issuer's business combination (the &quot;Merger&quot;) with what was then known as &quot;Acer Therapeutics Inc.&quot; (&quot;Private Acer&quot;) in accordance with the terms of the Agreement and Plan of Merger and Reorganization dated June 30, 2017 among the Issuer, Opexa Merger Sub, Inc. and Private Acer, in exchange for 1,750,000 shares of common stock of Private Acer.</footnote>
    </footnotes>

    <ownerSignature>
        <signatureName>/s/ Daniel S. Clevenger, Attorney-in-Fact for Chris Schelling</signatureName>
        <signatureDate>2017-09-21</signatureDate>
    </ownerSignature>
</ownershipDocument>
