Dofequidar fumarate(MS-209 fumarate), an orally active quinoline compound, has been reported to overcome MDR by inhibiting ABCB1/P-gp, ABCC1/MDR-associated protein 1, or both.

Dexrazoxane Hydrochloride

DDP-38003 dihydrochloride is an novel, orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with an IC50 of 84 nM.

Dasatinib (BMS-354825, Sprycel) is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of ＜1 nM, 0.5 nM and 79 nM, respectively.

CYT997 is a potent microtubule polymerization inhibitor with IC50 of 10-100 nM in cancer cell lines. Phase 1/2.

CKD-516 (Valecobulin, CKD516) is a potent beta-tubulin polymerization inhibitor with marked antitumor activity both in vitro and in vivo.

CB-1158 (INCB-01158) is a potent, selective, oral available Arginase inhibitor with IC50 of 98 nM.

Cabazitaxel (Jevtana, XRP6258) is a semi-synthetic derivative of a natural taxoid.

BSI-201 (Iniparib; NSC-746045) is a PARP1 inhibitor with demonstrated effectiveness in triple-negative breast cancer (TNBC).

BMS-906024 is a highly potent, selective inhibitor of γ-secretase mediated signaling of Notch1/2/3/4 receptors with IC50 of 1.6/0.7/3.4/2.9 nM, respectively.

BMS-794833 is a potent ATP competitive inhibitor of Met/VEGFR2 with IC50 of 1.7/15 nM; also inhibits Ron, Axl and Flt3 with IC50 of <3 nM; a prodrug of BMS-817378.

BGB-3111 is a potent, selective and orally available Bruton's tyrosine kinase (Btk) inhibitor.

BAY-1436032 (BAY1436032) is a potent, selective, orally available inhibitor of pan-mutant IDH1 with IC50 of 15 nM for both IDH1 R132H and R132C, respectively.

BAY 1143572 is a highly selective, potent and orally available inhibitor of PTEFb/CDK9; inhibits the proliferation of AML cell lines with a median IC50 of 385 nM.

BAY 1082439 is a highly selective and balanced PI3Kα/β inhibitor demonstrated potent activity in tumors with activated PI3Kα and loss-of-function of PTEN.

AZD4573 is a CDK9 inhibitor with an IC50 of <3 nM extracted from patent US 20160376287 A1, example 14.

AV-412(MP-412) is a potent dual inhibitor of EGFR and ErbB2(IC50=19 nM) tyrosine kinases, including the mutant EGFR(L858R IC50=0.51 nM, T790M IC50=0.79 nM); inhibits autophosphorylation of EGFR and ErbB2 with IC(50) of 43 and 282 nM, respectively.

AT7519 trifluoroacetate is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM; less potent to CDK3 and little active to CDK7.

AT-101 is a BH3 mimetic known to be a potent inhibitor of antiapoptotic Bcl-2 family members.

AST-1306 is a novel irreversible inhibitor of EGFR and ErbB2 with IC50 of 0.5 nM and 3 nM, also effective in mutation EGFR T790M/L858R, more potent to ErbB2-overexpressing cells, 3000-fold selective for ErbB family than other kinases.

ARRY-334543 is a small molecule inhibitor of ErbB1 and ErbB2 tyrosine kinases.

APTO-253 is a novel small molecule with potent anti-tumor activity in cancer cells via induction of the gene that expresses the Krüppel-like factor 4 (KLF4) master transcription factor, leading to cell cycle inhibition and programmed cell death.

An orally available thioxanthone-based DNA intercalator and inhibitor of the DNA repair enzyme apurinic-apyrimidinic endonuclease 1 (APE1) potential antineoplastic activity, also inhibits autophagy.

Amonafide(AS1413) produces protein-associated DNA-strand breaks through a topoisomerase II-mediated reaction, but does not produce topoisomerase I-mediated DNA cleavage.

AMG232 is a potent, selective and orally bioavailable inhibitor of MDM2−p53 interaction with IC50 value of 9.1 nM in EdU cells .

Akt1 and Akt2-IN-1 is an allosteric inhibitor of Akt1 (IC50 = 3.5 nM) and Akt2 (IC50 = 42 nM), with potent and balanced activity.

Abiraterone (CB-7598) is a potent CYP17 inhibitor with IC50 of 2 nM.

A potent, specific, orally available, ATP‑competitive inhibitor of Chk1 and Chk2 with Ki of 2.2 nM and 0.07 nM, respectively.

A potent, selective, irreversible EGFR mutants with IC50 of 12, 3, 4 and 5 nM for EGFR L858R-T790M, Del-T790M, L858R, and EGFR Del, respectively.

A potent, selective and orally active Chk1 inhibitor.