ArQule Announces Closing of Public Offering and Full Exercise of Option to Purchase Additional Shares

ArQule, Inc. (Nasdaq: ARQL) today announced the closing of its previously announced underwritten public offering of common stock, including the exercise in full by the underwriters of their option to purchase an additional 1,650,000 shares at the public offering price of $5.50 per share. The exercise of the option to purchase additional shares brought the total number of shares of common stock sold by ArQule to 12,650,000 shares and increased the gross proceeds raised in the offering, before deducting underwriting discounts and commissions and estimated expenses of the offering payable by ArQule, to approximately $70 million.

The Company intends to use the net proceeds of the offering to fund its core clinical programs and for general corporate purposes.

Leerink Partners acted as sole book-running manager for the offering. Needham & Company, LLC acted as lead co-manager, and Roth Capital Partners, B. Riley FBR and JonesTrading Institutional Services LLC acted as co-managers for the offering.

The securities described above were offered by ArQule pursuant to an effective shelf registration statement on Form S-3 (File. No. 333-213456), including a base prospectus, that was previously filed by ArQule with the Securities and Exchange Commission ("SEC”). A final prospectus supplement and accompanying prospectus relating to the offering filed with the SEC is available on the SEC’s website located at www.sec.gov or on ArQule’s website, www.arqule.com. Copies of the final prospectus supplement and the accompanying prospectus relating to the offering may be obtained from Leerink Partners LLC, Attention: Syndicate Department, One Federal Street, 37^th Floor, Boston, MA 02110, by telephone at (800) 808-7525, ext. 6132 or by email at syndicate@leerink.com.

This press release does not constitute an offer to sell or a solicitation of an offer to buy, nor will there be any sales of these securities in any jurisdiction in which such offer, solicitation or sale would be unlawful prior to registration or qualification under the securities laws of such jurisdiction.

About ArQule

ArQule is a biopharmaceutical company engaged in the research and development of targeted therapeutics to treat cancers and rare diseases. ArQule’s mission is to discover, develop and commercialize novel small molecule drugs in areas of high unmet need that will dramatically extend and improve the lives of our patients. Our clinical-stage pipeline consists of five drug candidates, all of which are in targeted, biomarker-defined patient populations, making ArQule a leader among companies our size in precision medicine. ArQule’s pipeline includes: ARQ 531, an orally bioavailable, potent and reversible inhibitor of both wild type and C481S-mutant BTK, in a Phase 1 trial for patients with B-cell malignancies refractory to other therapeutic options; Miransertib (ARQ 092), a selective inhibitor of the AKT serine/threonine kinase, in a phase 1/2 company-sponsored trial for Overgrowth Diseases, in a Phase 1 trial for ultra-rare Proteus syndrome conducted by the National Institutes of Health (NIH), and in a Phase 1b trial in combination with the hormonal therapy, anastrozole, in patients with advanced endometrial cancer; ARQ 751 a next generation AKT inhibitor, in a Phase 1 trial for patients with AKT1 and PI3K mutations; Derazantinib, a multi-kinase inhibitor designed to preferentially inhibit the fibroblast growth factor receptor (FGFR) family, in a registrational trial for iCCA; and ARQ 761, a ß-lapachone analog being evaluated as a promoter of NQO1-mediated programmed cancer cell necrosis, in a Phase 1/2 trial in multiple oncology indications in partnership with the University of Texas Southwestern Medical Center. ArQule’s current discovery efforts are focused on the identification and development of novel kinase inhibitors, leveraging the Company’s proprietary library of compounds.

Forward Looking Statements

This press release contains forward-looking statements including, without limitation, statements about ArQule’s expectations regarding, among other things, the expected use of proceeds. These statements are based on ArQule’s current beliefs and expectations, and involve assumptions that may never materialize or may prove to be incorrect. Actual results and the timing of events could differ materially from those anticipated in such forward-looking statements as a result of various risks and uncertainties, which include risks and uncertainties associated with ArQule’s drug development and other activities. For more detailed information about these risks and uncertainties, see ArQule’s periodic reports filed with the SEC. ArQule does not undertake any obligation to publicly update any forward-looking statements.

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