| DC75395 |
CA-170 free base |
CA-170, also known as AUPM170 and PD-1-IN-17, is a programmed cell death-1 (PD-1) inhibitor. PD-1-IN-17 was first reported in patent WO2015033301A1, (Compound 4), inhibits 92% splenocyte proliferation at 100 nM. |
|
| DC75396 |
Bendamustine HCl |
Bendamustine hydrochloride is the hydrochloride salt of bendamustine, a bifunctional mechlorethamine derivative with alkylator and antimetabolite activities. Bendamustine possesses three active moieties: an alkylating group; a benzimidazole ring, which may act as a purine analogue; and a butyric acid side chain. Although its exact mechanism of action is unknown, this agent appears to act primarily as an alkylator. Bendamustine metabolites alkylate and crosslink macromolecules, resulting in DNA, RNA and protein synthesis inhibition, and, subsequently, apoptosis. In October 2008, the FDA granted further approval to market Treanda for the treatment of indolent B-cell non-Hodgkin's lymphoma (NHL) that has progressed during or within six months of treatment with rituximab or a rituximab-containing regimen. |
|
| DC75397 |
Copanlisib free base |
Copanlisib, also known as BAY 80-6946, is a potent phosphoinositide 3-kinase (PI3K) inhibitor. Copanlisib inhibits the activation of the PI3K signaling pathway, which may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Activation of the PI3K signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K signaling may contribute to tumor resistance to a variety of antineoplastic agents. Copanlisib was approved for the treatment of adult patients experiencing relapsed follicular lymphoma who have received at least two prior systemic therapies. |
|
| DC75398 |
Buparlisib (BKM120) |
Buparlisib, also known as BKM120, is an orally bioavailable specific oral inhibitor of the pan-class I phosphatidylinositol 3-kinase (PI3K) family of lipid kinases with potential antineoplastic activity. PI3K inhibitor BKM120 specifically inhibits class I PIK3 in the PI3K/AKT kinase (or protein kinase B) signaling pathway in an ATP-competitive manner, thereby inhibiting the production of the secondary messenger phosphatidylinositol-3,4,5-trisphosphate and activation of the PI3K signaling pathway. |
|
| DC75399 |
Baricitinib |
Baricitinib, also known as INCB028050 or LY3009104, is a selective orally bioavailable JAK1/JAK2 inhibitor with nanomolar potency against JAK1 (5.9 nM) and JAK2 (5.7 nM). INCB028050 inhibits intracellular signaling of multiple proinflammatory cytokines including IL-6 and IL-23 at concentrations <50 nM. INCB028050 was also effective in multiple murine models of arthritis, with no evidence of suppression of humoral immunity or adverse hematologic effects. Baricitinib was approved for the treatment of rheumatoid arthritis (RA) in the United States. |
|
| DC75400 |
Apalutamide (ARN-509) |
Apalutamide, also known as ARN-509 and JNJ-56021927 , is an androgen receptor antagonist with potential antineoplastic activity. ARN-509 binds to AR in target tissues thereby preventing androgen-induced receptor activation and facilitating the formation of inactive complexes that cannot be translocated to the nucleus. This prevents binding to and transcription of AR-responsive genes. This ultimately inhibits the expression of genes that regulate prostate cancer cell proliferation and may lead to an inhibition of cell growth in AR-expressing tumor cells. |
|
| DC75401 |
CX4945 (Silmitasertib) |
Silmitasertib, also know as CX-4945, is an orally bioavailable small-molecule inhibitor of CK2 with potential antineoplastic activity. CK2 inhibitor CX-4945 selectively binds to and inhibits the enzyme casein kinase II (CK2), which may lead to an inhibition of cellular proliferation. CK2, a protein kinase often overexpressed in a variety of cancer cell types, appears to be correlated with malignant transformation, tumor growth and survival. |
|
| DC75402 |
Talazoparib |
Talazoparib, also known as BMN-673 and MDV-3800, is an orally bioavailable inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) with potential antineoplastic activity (PARP1 IC50 = 0.57 nmol/L). Talazoparib acts as an inhibitor of poly ADP ribose polymerase(PARP) which aids in single strand DNA repair. Cells that have BRCA1/2 mutations are susceptible to the cytotoxic effects of PARP inhibitors because of an accumulation of DNA damage. Talazoparib is theorized to have a higher potency than olaparib due to the additional mechanism of action called PARP trapping. PARP trapping is the mechanism of action where the PARP molecule is trapped on the DNA, which interferes with the cells ability to replicate. Talazoparib is found to be ~100 fold more efficient in PARP trapping than olaparib. Talazoparib was approved in 2018 by FDA. |
|
| DC75403 |
Abrocitinib |
Abrocitinib, also known as PF-04965842, is an oral Janus Kinase 1 inhibitor being investigated for treatment of plaque psoriasis. In January 2022, FDA approved abrocitinib for adults with moderate-to-severe atopic dermatitis. Abrocitinib at a dose of either 200 mg or 1 g once daily resulted in significantly greater reductions in signs and symptoms of moderate-to-severe atopic dermatitis than placebo at weeks 12 and 16. The 200-mg dose, but not the 100-mg dose, of abrocitinib was superior to dupilumab with respect to itch response at week 2. |
|
| DC75404 |
Abaperidone free base |
Abaperidone, also known as FI 8602, is an atypical antipsychotic. Reduced hsp70 in the prefrontal cortex may play a critical role in the etiology of many schizophrenia symptoms and may be linked to an atypical profile of antipsychotics, such as abaperidone. |
|
| DC75405 |
Birabresib |
Birabresib, also known as OTX015 and MK-8628, a potent BET bromodomian inhibitor, which targets the BET bromodomain proteins 2, 3, and 4 (BRD2/3/4). BRDs 2, 3, and 4 are considered potential cancer targets because of their pivotal role in regulating the transcription of growth-promoting genes and cell cycle regulators. OTX015 is the first BRD2/3/4 inhibitor to enter clinical trials. OTX015 showed antiproliferative activity in a large panel of cell lines derived from mature B-cell lymphoid tumors with median IC50 of 240 nmol/L, without significant differences among the different histotypes. |
|
| DC75406 |
AVN-101 HCl |
AVN-101 is a very potent 5-HT7 receptor antagonist, with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors. It is a milti-target drug candidate for the treatment of CNS disorders. |
|
| DC75407 |
Bazedoxifene acetate |
Bazedoxifene, also known as WAY-140424, is a third generation selective estrogen receptor modulator (SERM), developed by Pfizer following the completion of their takeover of Wyeth Pharmaceuticals. In late 2013, Pfizer received approval for bazedoxifene as part of the combination drug DUAVEE in the prevention (not treatment) of postmenopausal osteoporosis. Bazedoxifene is an indole-based ER ligand that binds to both ERα (IC50 = 26 nM) and ERβ (IC50 = 99 nM). |
|
| DC75408 |
Mirogabalin free base |
Mirogabalin, also known as DS-5565, is an α2δ-1 ligand being developed for pain associated with diabetic peripheral neuropathy, fibromyalgia, and postherpetic neuralgia. Mirogabalin was estimated to be 17-fold more potent than pregabalin. Mirogabalin is being developed by Daiichi Sankyo and related to drugs such as gabapentin and pregabalin. Similarly to these drugs, mirogabalin binds to the α2δ calcium channels (1 and 2), but with significantly higher potency than pregabalin. It has shown promising results in Phase II clinical trials for the treatment of diabetic peripheral neuropathic pain. |
|
| DC75409 |
Ibipinabant |
Ibipinabant, also known as BMS-646256, JD-5001 and SLV-319, is a potent and highly selective CB1 antagonist. It has potent anorectic effects in animals, and was researched for the treatment of obesity, although CB1 antagonists as a class have now fallen out of favour as potential anorectics following the problems seen with rimonabant, and so ibipinabant is now only used for laboratory research, especially structure-activity relationship studies into novel CB1 antagonists. |
|
| DC75410 |
(S,R,S)-AHPC HCl |
(S,R,S)-AHPC , also known as also known as MDK7526; VHL Ligand 1; Protein degrader 1, is a potent and selective protein degrader. MDK7526 has CAS#1448297-52-6, its HCl salt has CAS#1448189-80-7. MDK7526 is potential useful for the targeted degradation of the androgen receptor. MDK7526 binds androgen receptor such that androgen receptor is placed in proximity to the ubiquitin ligase to effect degrdn. (and inhibition) of androgen receptor. |
|
| DC75411 |
AZD-5153 HNT salt |
AZD-5153 HNT salt, is a 6-hydroxy-2-naphthoic acid salt of AZD-5153. AZD 5153 a potetn and selective orally available, bivalent inhibitor of the bromodomain and extraterminal (BET) protein BRD4 (IC50 = 5 nM). AZD5153 is highly Active against Hematologic Malignancies. |
|
| DC75412 |
GBR-12935 HCl |
GBR-12935 is a piperazine derivative which is a potent and selective dopamine reuptake inhibitor. It was originally developed in its 3H radiolabelled form for the purpose of mapping the distribution of dopaminergic neurons in the brain by selective labelling of dopamine transporter proteins. This has led to potential clinical uses in the diagnosis of Parkinson's disease, although selective radioligands such as Ioflupane (¹²³I) are now available for this application. GBR-12935 is now widely used in animal research into Parkinson's disease and the dopamine pathways in the brain. |
|
| DC75413 |
GBR-12935 free base |
GBR-12935 is a piperazine derivative which is a potent and selective dopamine reuptake inhibitor. It was originally developed in its 3H radiolabelled form for the purpose of mapping the distribution of dopaminergic neurons in the brain by selective labelling of dopamine transporter proteins. This has led to potential clinical uses in the diagnosis of Parkinson's disease, although selective radioligands such as Ioflupane (¹²³I) are now available for this application. GBR-12935 is now widely used in animal research into Parkinson's disease and the dopamine pathways in the brain. |
|
| DC75414 |
Eflornithine HCl hydrate |
Eflornithine, also known as Difluoromethylornithine, is a difluoromethylated ornithine compound with antineoplastic activity. Eflornithine irreversibly inhibits ornithine decarboxylase, an enzyme required for polyamine biosynthesis, thereby inhibiting the formation and proliferation of tumor cells. Polyamines are involved in nucleosome oligomerization and DNA conformation, creating a chromatin environment that stimulates neoplastic transformation of cells. This agent has been shown to induce apoptosis in leiomyoma cells. |
|
| DC75415 |
RN9893 |
RN-9893 is a potent and selective antagonist of the Transient Receptor Potential ion channel TRPV4. RN-9893 has IC50 values of 420 nM, 660 nM, and 320 nM for human, rat and mouse TRPV4 receptors, respectively. RN-9893 shows excellent selectivity over related TRP receptors with no inhibition of TRPV1 at a concentration of 10 μM, an IC50 >30 μM against TRPV3, an IC50 of approximately 30 μM against TRPM8, and also good selectivity using 54 binding assays against common biological targets. |
|
| DC75416 |
Anamorelin HCl |
Anamorelin, also known as RC-1291 or ONO-7643, is the orally bioavailable, small-molecule ghrelin mimetic with appetite-stimulating and anabolic activities. Anamorelin binds to and stimulates the growth hormone secretagogue receptor (GHSR) centrally, thereby mimicking the appetite-stimulating and growth hormone-releasing effects of grhelin. Stimulation of GHSR may also reduce the production of the pro-inflammatory cytokines TNF-alpha and interleukin-6, which may play a direct role in cancer-related loss of appetite. |
|
| DC75417 |
Amsacrine HCl |
Amsacrine is an aminoacridine derivative with potential antineoplastic activity. Although its mechanism of action is incompletely defined, amsacrine may intercalate into DNA and inhibit topoisomerase II, resulting in DNA double-strand breaks, arrest of the S/G2 phase of the cell cycle, and cell death. This agent's cytotoxicity is maximal during the S phase of the cell cycle when topoisomerase levels are greatest. In addition, amsacrine may induce transcription of tumor promoter p53 protein and block p53 ubiquitination and proteasomal degradation, resulting in p53-dependent tumor cell apoptosis. |
|
| DC75418 |
Cerdulatinib free base |
Cerdulatinib, also known as PRT2070 and PRT062070, is a n ovel, oral, dual spleen tyrosine kinase (Syk) and janus kinase (JAK) inhibitor. Cerdulatinib preferentially inhibited JAK1 and JAK3 dependent cytokine mediated signaling and functional responses in various cell types. IL2 mediated STAT5 Y694 was inhibited with an IC50 of 0.27μM, while IL4 mediated signaling to STAT6 Y641 and functional responses in B cells and monocytes, namely CD69, CD25, and CD23 up-regulation, were inhibited with IC50Â’s within the range of 0.11μM to 0.57μM. It is currently being studied in patients with genetically-defined hematologic cancers, as well as for patients who have failed therapy due to relapse or acquired mutations. |
|
| DC75419 |
Givinostat HCl hydrate |
Givinostat hydrochloride is a novel histone deacetylase inhibitor with potential anti-inflammatory, anti-angiogenic, and antineoplastic activities. |
|
| DC75420 |
Isoquercetin |
Isoquercetin, also known as Isoquercitrin, Quercetin 3-O-glucopyranoside, is a flavonoid, a type of chemical compound. It is the 3-O-glucoside of quercetin. Isoquercetin can be isolated from various plant species including Mangifera indica (mango) and Rheum nobile (the Noble rhubarb). It is also present in the leaves of Annona squamosa and Camellia sinensis (tea). Isoquercetin is presently being investigated for prevention of Thromboembolism in selected cancer patients (NCT02195232) and as an anti-fatigue agent in kidney cancer patients treated with sunitinib (NCT02446795). |
|
| DC75421 |
Afatinib dimaleate |
Afatinib dimaleate is an orally bioavailable dual receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity. EGFR/HER2 tyrosine kinase inhibitor BIBW 2992 irreversibly binds to and inhibits human epidermal growth factor receptors 1 and 2 (EGFR-1; HER2), which may result in the inhibition of tumor growth and angiogenesis. EGFR/HER2 are RTKs that belong to the EGFR superfamily; both play major roles in tumor cell proliferation and tumor vascularization and are overexpressed in many cancer cell types. Afatinib is approved in much of the world (including the United States, Canada, the United Kingdom and Australia) for the treatment of metastatic non-small cell lung carcinoma (NSCLC), developed by Boehringer Ingelheim. It acts as an angiokinase inhibitor. |
|
| DC75422 |
AEW-541 free base |
AEW541, also known as NVP-AEW541, is a novel, potent IGF-IR kinase inhibitor. NVP-AEW541 is capable of distinguishing between the IGF-IR (IC50 = 0.086 microM) and the closely related InsR (IC50 = 2.3 microM) in cells. NVP- AEW541 abrogates IGF-I-mediated survival and colony formation in soft agar at concentrations that are consistent with inhibition of IGF-IR autophosphorylation. Note: AEW541 has a Cis-configuration on the cyclobutane ring. Its CAS# is 475489-16-8. Many vendors and Sc-finder scholar made mistake - AEW541 was mistakenly listed as CAS#475488-34-7, the trans-isomer of AEW541. The correct structure of AEW541 can be confirmed from Joel Slade, et al (from Novartis), Org. Process Res. Dev. 2007, 11, 5, 825–835. |
|
| DC75423 |
Acotiamide hydrochloride trihydrate |
Acotiamide, also known as YM-443 and Z-338, is a drug approved in Japan for the treatment of postprandial fullness, upper abdominal bloating, and early satiation due to functional dyspepsia. It acts as an acetylcholinesterase inhibitor. Note: The Approved drug API is a cotiamide HCl trihydrate (1:1:3) |
|
| DC75424 |
AC480 HCl |
AC480, also known as BMS-599626, is an orally bioavailable inhibitor of the HER1, HER2 and HER4 tyrosine kinases (IC50 =22, 32 and 190 nM, respectively) with potential antineoplastic activity. BMS-599626 inhibits human epidermal growth factor receptors (HER) HER1, HER2 and HER4, thereby inhibiting the proliferation of tumor cells that overexpress these receptors. |
|
