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

    <schemaVersion>X0206</schemaVersion>

    <documentType>3</documentType>

    <periodOfReport>2016-01-14</periodOfReport>

    <noSecuritiesOwned>0</noSecuritiesOwned>

    <issuer>
        <issuerCik>0000895051</issuerCik>
        <issuerName>CASI Pharmaceuticals, Inc.</issuerName>
        <issuerTradingSymbol>CASI</issuerTradingSymbol>
    </issuer>

    <reportingOwner>
        <reportingOwnerId>
            <rptOwnerCik>0001663831</rptOwnerCik>
            <rptOwnerName>SPARKLE BYTE LTD</rptOwnerName>
        </reportingOwnerId>
        <reportingOwnerAddress>
            <rptOwnerStreet1>P.O. BOX 957</rptOwnerStreet1>
            <rptOwnerStreet2>OFFSHORE INCORPORATIONS CENTRE</rptOwnerStreet2>
            <rptOwnerCity>ROAD TOWN</rptOwnerCity>
            <rptOwnerState>D8</rptOwnerState>
            <rptOwnerZipCode></rptOwnerZipCode>
            <rptOwnerStateDescription>VIRGIN ISLANDS, BRITISH</rptOwnerStateDescription>
        </reportingOwnerAddress>
        <reportingOwnerRelationship>
            <isDirector>0</isDirector>
            <isOfficer>0</isOfficer>
            <isTenPercentOwner>1</isTenPercentOwner>
            <isOther>0</isOther>
            <officerTitle></officerTitle>
            <otherText></otherText>
        </reportingOwnerRelationship>
    </reportingOwner>

    <reportingOwner>
        <reportingOwnerId>
            <rptOwnerCik>0001663833</rptOwnerCik>
            <rptOwnerName>SNOW MOON LTD</rptOwnerName>
        </reportingOwnerId>
        <reportingOwnerAddress>
            <rptOwnerStreet1>P.O. BOX 957</rptOwnerStreet1>
            <rptOwnerStreet2>OFFSHORE INCORPORATIONS CENTRE</rptOwnerStreet2>
            <rptOwnerCity>ROAD TOWN</rptOwnerCity>
            <rptOwnerState>D8</rptOwnerState>
            <rptOwnerZipCode></rptOwnerZipCode>
            <rptOwnerStateDescription>VIRGIN ISLANDS, BRITISH</rptOwnerStateDescription>
        </reportingOwnerAddress>
        <reportingOwnerRelationship>
            <isDirector>0</isDirector>
            <isOfficer>0</isOfficer>
            <isTenPercentOwner>1</isTenPercentOwner>
            <isOther>0</isOther>
            <officerTitle></officerTitle>
            <otherText></otherText>
        </reportingOwnerRelationship>
    </reportingOwner>

    <reportingOwner>
        <reportingOwnerId>
            <rptOwnerCik>0001664019</rptOwnerCik>
            <rptOwnerName>TIANJIN JINGRAN MANAGEMENT CENTER (LIMITED PARTNERSHIP)</rptOwnerName>
        </reportingOwnerId>
        <reportingOwnerAddress>
            <rptOwnerStreet1>RM 1704-4920 KUANG SHI GUO JI TOWER A</rptOwnerStreet1>
            <rptOwnerStreet2>XIANGLUOWAN BUSINESS CTR FREE TRADE ZONE</rptOwnerStreet2>
            <rptOwnerCity>TIANJIN</rptOwnerCity>
            <rptOwnerState>F4</rptOwnerState>
            <rptOwnerZipCode></rptOwnerZipCode>
            <rptOwnerStateDescription>CHINA</rptOwnerStateDescription>
        </reportingOwnerAddress>
        <reportingOwnerRelationship>
            <isDirector>0</isDirector>
            <isOfficer>0</isOfficer>
            <isTenPercentOwner>1</isTenPercentOwner>
            <isOther>0</isOther>
            <officerTitle></officerTitle>
            <otherText></otherText>
        </reportingOwnerRelationship>
    </reportingOwner>

    <reportingOwner>
        <reportingOwnerId>
            <rptOwnerCik>0001664018</rptOwnerCik>
            <rptOwnerName>HE XIE AI QI INVESTMENT MANAGEMENT (BEIJING) CO., LTD.</rptOwnerName>
        </reportingOwnerId>
        <reportingOwnerAddress>
            <rptOwnerStreet1>ROOM 5835, 5/F, SHENCHANG BUILDING</rptOwnerStreet1>
            <rptOwnerStreet2>51 ZHICHUN ROAD, HAIDIAN DISTRICT</rptOwnerStreet2>
            <rptOwnerCity>BEIJING</rptOwnerCity>
            <rptOwnerState>F4</rptOwnerState>
            <rptOwnerZipCode></rptOwnerZipCode>
            <rptOwnerStateDescription>CHINA</rptOwnerStateDescription>
        </reportingOwnerAddress>
        <reportingOwnerRelationship>
            <isDirector>0</isDirector>
            <isOfficer>0</isOfficer>
            <isTenPercentOwner>1</isTenPercentOwner>
            <isOther>0</isOther>
            <officerTitle></officerTitle>
            <otherText></otherText>
        </reportingOwnerRelationship>
    </reportingOwner>

    <reportingOwner>
        <reportingOwnerId>
            <rptOwnerCik>0001664022</rptOwnerCik>
            <rptOwnerName>Li Jianguang</rptOwnerName>
        </reportingOwnerId>
        <reportingOwnerAddress>
            <rptOwnerStreet1>6/F, TOWER A, COFCO PLAZA</rptOwnerStreet1>
            <rptOwnerStreet2>8 JIANGUOMENNEI AVENUE</rptOwnerStreet2>
            <rptOwnerCity>BEIJING</rptOwnerCity>
            <rptOwnerState>F4</rptOwnerState>
            <rptOwnerZipCode></rptOwnerZipCode>
            <rptOwnerStateDescription>CHINA</rptOwnerStateDescription>
        </reportingOwnerAddress>
        <reportingOwnerRelationship>
            <isDirector>0</isDirector>
            <isOfficer>0</isOfficer>
            <isTenPercentOwner>1</isTenPercentOwner>
            <isOther>0</isOther>
            <officerTitle></officerTitle>
            <otherText></otherText>
        </reportingOwnerRelationship>
    </reportingOwner>

    <reportingOwner>
        <reportingOwnerId>
            <rptOwnerCik>0001664036</rptOwnerCik>
            <rptOwnerName>Lin Dongliang</rptOwnerName>
        </reportingOwnerId>
        <reportingOwnerAddress>
            <rptOwnerStreet1>6/F, TOWER A, COFCO PLAZA</rptOwnerStreet1>
            <rptOwnerStreet2>8 JIANGUOMENNEI AVENUE</rptOwnerStreet2>
            <rptOwnerCity>BEIJING</rptOwnerCity>
            <rptOwnerState>F4</rptOwnerState>
            <rptOwnerZipCode></rptOwnerZipCode>
            <rptOwnerStateDescription>CHINA</rptOwnerStateDescription>
        </reportingOwnerAddress>
        <reportingOwnerRelationship>
            <isDirector>0</isDirector>
            <isOfficer>0</isOfficer>
            <isTenPercentOwner>1</isTenPercentOwner>
            <isOther>0</isOther>
            <officerTitle></officerTitle>
            <otherText></otherText>
        </reportingOwnerRelationship>
    </reportingOwner>

    <reportingOwner>
        <reportingOwnerId>
            <rptOwnerCik>0001663830</rptOwnerCik>
            <rptOwnerName>Yang Fei</rptOwnerName>
        </reportingOwnerId>
        <reportingOwnerAddress>
            <rptOwnerStreet1>34/F SOUTH TOWER, POLY INTERNATIONAL PLZ</rptOwnerStreet1>
            <rptOwnerStreet2>1 EAST PAZHOUDADAO</rptOwnerStreet2>
            <rptOwnerCity>GUANGZHOU</rptOwnerCity>
            <rptOwnerState>F4</rptOwnerState>
            <rptOwnerZipCode></rptOwnerZipCode>
            <rptOwnerStateDescription>CHINA</rptOwnerStateDescription>
        </reportingOwnerAddress>
        <reportingOwnerRelationship>
            <isDirector>0</isDirector>
            <isOfficer>0</isOfficer>
            <isTenPercentOwner>1</isTenPercentOwner>
            <isOther>0</isOther>
            <officerTitle></officerTitle>
            <otherText></otherText>
        </reportingOwnerRelationship>
    </reportingOwner>

    <reportingOwner>
        <reportingOwnerId>
            <rptOwnerCik>0001664025</rptOwnerCik>
            <rptOwnerName>Zhang Suyang</rptOwnerName>
        </reportingOwnerId>
        <reportingOwnerAddress>
            <rptOwnerStreet1>RM 1105, AETNA TOWER, 107 ZUNYI RD</rptOwnerStreet1>
            <rptOwnerStreet2></rptOwnerStreet2>
            <rptOwnerCity>SHANGHAI</rptOwnerCity>
            <rptOwnerState>F4</rptOwnerState>
            <rptOwnerZipCode></rptOwnerZipCode>
            <rptOwnerStateDescription>CHINA</rptOwnerStateDescription>
        </reportingOwnerAddress>
        <reportingOwnerRelationship>
            <isDirector>0</isDirector>
            <isOfficer>0</isOfficer>
            <isTenPercentOwner>1</isTenPercentOwner>
            <isOther>0</isOther>
            <officerTitle></officerTitle>
            <otherText></otherText>
        </reportingOwnerRelationship>
    </reportingOwner>

    <reportingOwner>
        <reportingOwnerId>
            <rptOwnerCik>0001664109</rptOwnerCik>
            <rptOwnerName>Shong Hugo</rptOwnerName>
        </reportingOwnerId>
        <reportingOwnerAddress>
            <rptOwnerStreet1>6/F, TOWER A, COFCO PLAZA</rptOwnerStreet1>
            <rptOwnerStreet2>8 JIANGUOMENNEI AVENUE</rptOwnerStreet2>
            <rptOwnerCity>BEIJING</rptOwnerCity>
            <rptOwnerState>F4</rptOwnerState>
            <rptOwnerZipCode></rptOwnerZipCode>
            <rptOwnerStateDescription>CHINA</rptOwnerStateDescription>
        </reportingOwnerAddress>
        <reportingOwnerRelationship>
            <isDirector>0</isDirector>
            <isOfficer>0</isOfficer>
            <isTenPercentOwner>1</isTenPercentOwner>
            <isOther>0</isOther>
            <officerTitle></officerTitle>
            <otherText></otherText>
        </reportingOwnerRelationship>
    </reportingOwner>

    <nonDerivativeTable>
        <nonDerivativeHolding>
            <securityTitle>
                <value>Common Stock</value>
            </securityTitle>
            <postTransactionAmounts>
                <sharesOwnedFollowingTransaction>
                    <value>4744910</value>
                </sharesOwnedFollowingTransaction>
            </postTransactionAmounts>
            <ownershipNature>
                <directOrIndirectOwnership>
                    <value>D</value>
                    <footnoteId id="F1"/>
                </directOrIndirectOwnership>
            </ownershipNature>
        </nonDerivativeHolding>
    </nonDerivativeTable>

    <derivativeTable>
        <derivativeHolding>
            <securityTitle>
                <value>Warrant</value>
            </securityTitle>
            <conversionOrExercisePrice>
                <value>1.69</value>
            </conversionOrExercisePrice>
            <exerciseDate>
                <value>2016-04-14</value>
            </exerciseDate>
            <expirationDate>
                <value>2019-04-14</value>
            </expirationDate>
            <underlyingSecurity>
                <underlyingSecurityTitle>
                    <value>Common Stock</value>
                </underlyingSecurityTitle>
                <underlyingSecurityShares>
                    <value>948982</value>
                </underlyingSecurityShares>
            </underlyingSecurity>
            <ownershipNature>
                <directOrIndirectOwnership>
                    <value>D</value>
                    <footnoteId id="F1"/>
                </directOrIndirectOwnership>
            </ownershipNature>
        </derivativeHolding>
    </derivativeTable>

    <footnotes>
        <footnote id="F1">These securities are directly owned by Sparkle Byte Limited (&quot;Sparkle Byte&quot;) and may be deemed to be indirectly beneficially owned by the other reporting persons. Snow Moon Limited (&quot;Snow Moon&quot;) holds 100% of the equity interest of Sparkle Byte. Tianjin Jingran Management Center (Limited Partnership) (&quot;Tianjin Jingran&quot;) holds 100% of the equity interest of Snow Moon. He Xie Ai Qi Investment Management (Beijing) Co., Ltd. (&quot;He Xie Ai Qi&quot;) is the general partner of Tianjin Jingran. Jianguang Li, Dongliang Lin, Fei Yang and Suyang Zhang each holds 25% of the equity interest of He Xie Ai Qi. Jianguang Li, Dongliang Lin and Hugo Shong are the directors of He Xie Ai Qi. The filing of this statement by the reporting persons shall not be deemed an admission that such persons are, for purposes of Section 16 of the Securities and Exchange Act of 1934 or otherwise, the beneficial owner of any equity securities covered by this statement.</footnote>
    </footnotes>

    <ownerSignature>
        <signatureName>/s/ Dongliang Lin, Director, on behalf of Sparkle Byte Limited</signatureName>
        <signatureDate>2016-01-22</signatureDate>
    </ownerSignature>

    <ownerSignature>
        <signatureName>/s/ Dongliang Lin, Director, on behalf of Snow Moon Limited</signatureName>
        <signatureDate>2016-01-22</signatureDate>
    </ownerSignature>

    <ownerSignature>
        <signatureName>/s/ Qiuyue Zhong, Representative, on behalf of Tianjin Jingran Management Center (Limited Partnership)</signatureName>
        <signatureDate>2016-01-22</signatureDate>
    </ownerSignature>

    <ownerSignature>
        <signatureName>/s/ Hugo Shong, Director, on behalf of He Xie Ai Qi Investment Management (Beijing) Co., Ltd.</signatureName>
        <signatureDate>2016-01-22</signatureDate>
    </ownerSignature>

    <ownerSignature>
        <signatureName>/s/ Jianguang Li</signatureName>
        <signatureDate>2016-01-25</signatureDate>
    </ownerSignature>

    <ownerSignature>
        <signatureName>/s/ Dongliang Lin</signatureName>
        <signatureDate>2016-01-25</signatureDate>
    </ownerSignature>

    <ownerSignature>
        <signatureName>/s/ Fei Yang</signatureName>
        <signatureDate>2016-01-25</signatureDate>
    </ownerSignature>

    <ownerSignature>
        <signatureName>/s/ Suyang Zhang</signatureName>
        <signatureDate>2016-01-25</signatureDate>
    </ownerSignature>

    <ownerSignature>
        <signatureName>/s/ Hugo Shong</signatureName>
        <signatureDate>2016-01-25</signatureDate>
    </ownerSignature>
</ownershipDocument>
