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, 37th
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 ?-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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