Cell Cycle includes many processes necessary for successful self-replication, and consists of DNA synthesis (S) and mitosis (M) phases separated by gap phases in the order G1–S–G2–M. S phase and M phase are usually separated by gap phases called G1 and G2, when cell-cycle progression can be regulated by various intracellular and extracellular signals. In order to move from one phase of its life cycle to the next, a cell must pass through numerous checkpoints. At each checkpoint, specialized proteins determine whether the necessary conditions exist. Progression through G1 phase is controlled by pRB proteins, and phosphorylation of pRB proteins by CDKs releases E2F factors, promoting the transition to S phase. The G2/M transition that commits cells to division is a default consequence of initiating the cell cycle at the G1/S transition, many proteins, such Wee1, PLK1 and cdc25, is involved the regulation of this process. The best-understood checkpoints are those activated by DNA damage and problems with DNA replication.

DNA damage response (DDR) is a series of regulatory events including DNA damage, cell-cycle arrest, regulation of DNA replication, and repair or bypass of DNA damage to ensure the maintenance of genomic stability and cell viability. Genome instability arises if cells initiate mitosis when chromosomes are only partially replicated or are damaged by a double-strand DNA break (DSB). To prevent cells with damaged DNA from entering mitosis, ATR inhibits cyclin B/Cdk1 activation by stimulating the Cdk1 inhibitory kinase Wee1 and inhibiting Cdc25C via Chk1, besides, ATM and ATR also initiate DNA repair by phosphorylating several other substrates.

In cancer cells, the cell cycle regulators as well as other elements of the DDR pathway have been found to protect tumor cells from different stresses and to promote tumor progression. Thus, cell cycle proteins that directly regulate cell cycle progression (such as CDKs), as well as checkpoint kinases, Aurora kinases and PLKs, are promising targets in cancer therapy.

References:
[1] Rhind N, et al. Cold Spring Harb Perspect Biol. 2012 Oct; 4(10): a005942.
[2] Duronio RJ, et al. Cold Spring Harb Perspect Biol. 2013 Mar; 5(3): a008904.
[3] Liu W, et al. Mol Cancer. 2017 Mar 14;16(1):60.
[4] Ghelli Luserna di Rora' A, et al. J Hematol Oncol. 2017 Mar 29;10(1):77.


Anti-infection >
Arenavirus Bacterial CMV Enterovirus Filovirus Fungal HBV HCV HIV HSV Influenza Virus Parasite Reverse Transcriptase RSV SARS-CoV
Antibody-drug Conjugate >
ADC Cytotoxin ADC Linker Drug-Linker Conjugates for ADC PROTAC-linker Conjugate for PAC
Apoptosis >
Apoptosis Bcl-2 Family c-Myc Caspase DAPK Ferroptosis IAP MDM-2/p53 PKD RIP kinase Survivin Thymidylate Synthase TNF Receptor
Autophagy >
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Antifolate APC ATM/ATR Aurora Kinase Casein Kinase CDK Checkpoint Kinase (Chk) CRISPR/Cas9 Deubiquitinase DNA Alkylator/Crosslinker DNA-PK DNA/RNA Synthesis Eukaryotic Initiation Factor (eIF) G-quadruplex Haspin Kinase HDAC HSP IRE1 Kinesin LIM Kinase (LIMK) Microtubule/Tubulin Mps1 Nucleoside Antimetabolite/Analog p97 PAK PARP PERK Polo-like Kinase (PLK) PPAR RAD51 ROCK Sirtuin SRPK Telomerase TOPK Topoisomerase Wee1
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ERK JNK KLF MAP3K MAP4K MAPKAPK2 (MK2) MEK Mixed Lineage Kinase MNK p38 MAPK Raf Ribosomal S6 Kinase (RSK)
Membrane Transporter/Ion Channel >
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Metabolic Enzyme/Protease >
15-PGDH 5 alpha Reductase 5-Lipoxygenase Acetyl-CoA Carboxylase Acyltransferase Adenosine Deaminase Adenosine Kinase Aldehyde Dehydrogenase (ALDH) Aldose Reductase Aminopeptidase Angiotensin-converting Enzyme (ACE) ATGL ATP Citrate Lyase Carbonic Anhydrase Carboxypeptidase Cathepsin CETP COMT Cytochrome P450 Dipeptidyl Peptidase Dopamine β-hydroxylase E1/E2/E3 Enzyme Elastase Enolase FAAH FABP Factor Xa Farnesyl Transferase Fatty Acid Synthase (FAS) FXR Glucokinase GSNOR Gutathione S-transferase HCV Protease Hexokinase HIF/HIF Prolyl-Hydroxylase HIV Integrase HIV Protease HMG-CoA Reductase (HMGCR) HSP Indoleamine 2,3-Dioxygenase (IDO) Isocitrate Dehydrogenase (IDH) Lactate Dehydrogenase LXR MAGL Mineralocorticoid Receptor Mitochondrial Metabolism MMP Nampt NEDD8-activating Enzyme Neprilysin PAI-1 PDHK PGC-1α Phosphatase Phosphodiesterase (PDE) Phospholipase Procollagen C Proteinase Proteasome Pyruvate Kinase RAR/RXR Renin ROR Ser/Thr Protease SGK Stearoyl-CoA Desaturase (SCD) Thrombin Tryptophan Hydroxylase Tyrosinase Xanthine Oxidase
Neuronal Signaling >
5-HT Receptor AChE Adenosine Kinase Amyloid-β Beta-secretase CaMK CGRP Receptor COMT Dopamine Receptor Dopamine Transporter FAAH GABA Receptor GlyT iGluR Imidazoline Receptor mAChR Melatonin Receptor Monoamine Oxidase nAChR Neurokinin Receptor Opioid Receptor Serotonin Transporter γ-secretase
NF-κB >
NF-κB IKK Keap1-Nrf2 MALT1
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Akt AMPK ATM/ATR DNA-PK GSK-3 MELK mTOR PDK-1 PI3K PI4K PIKfyve PTEN
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Casein Kinase ERK Gli GSK-3 Hedgehog Hippo (MST) JAK Notch Oct3/4 PKA Porcupine ROCK sFRP-1 Smo STAT TGF-beta/Smad Wnt YAP β-catenin γ-secretase
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VD/VDR
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2'-Deoxy-2'-fluoro-L-uridine

2'-Deoxy-2'-fluoro-l-uridine is an L-nucleoside compound. 2'-Deoxy-2'-fluoro-l-uridine is a potent, selective viral RNA polymerase inhibitor, thereby inhibiting RNA virus replication[1].

  • CAS Number: 622785-69-7
  • MF: C9H11FN2O5
  • MW: 246.19200
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Cirtuvivint

Cirtuvivint (SM08502) is a potent and orally active CDC-like kinase (CLK) inhibitor. Cirtuvivint can be used for solid tumors research[1].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

4’-Azido-3’-O-benzoyl-5’-O-(m-chlorobenzoyl)-2’-deoxy-2’-fluoro-beta-D-arabinouridine

4’-Azido-3’-O-benzoyl-5’-O-(m-chlorobenzoyl)-2’-deoxy-2’-fluoro-beta-D-arabinouridine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].

  • CAS Number: 1333126-30-9
  • MF: C23H17ClFN5O7
  • MW: 529.86
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

9-(3-Deoxy-3-fluoro-β-D-ribofuranosyl)-6-(naphthalen-1-yl)purine

9-(3-Deoxy-3-fluoro-β-D-ribofuranosyl)-6-(naphthalen-1-yl)purine is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].

  • CAS Number: 1612191-92-0
  • MF:
  • MW:
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5-Methoxymethyluridine

5-Methoxymethyluridine is a thymidine analog. Analogs of this series have insertional activity towards replicated DNA. They can be used to label cells and track DNA synthesis[1].

  • CAS Number: 82448-44-0
  • MF: C11H16N2O7
  • MW: 288.25
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Silmitasertib (CX-4945)

CX-4945 is a potent, selective and oral casein kinase 2 (CK2) inhibitor with a Ki of 0.38 nM.

  • CAS Number: 1009820-21-6
  • MF: C19H12ClN3O2
  • MW: 349.771
  • Catalog: Autophagy
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 568.5±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 297.6±30.1 °C

Capecitabine-d11

Capecitabine-d11 is the deuterium labeled Capecitabine. Capecitabine is an oral prodrug that is converted to its active metabolite, 5-FU, by thymidine phosphorylase[1][2].

  • CAS Number: 1132662-08-8
  • MF: C15H11D11FN3O6
  • MW: 370.418
  • Catalog: Apoptosis
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-(1-Oxopropyl)cytidine

N-(1-Oxopropyl)cytidine is a cytidine analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities[1].

  • CAS Number: 60107-04-2
  • MF: C12H17N3O6
  • MW: 299.28
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2-Aminopurine-9-beta-D-(2'-deoxy-2'-fluoro)arabino-riboside

2-Amino-9-(2-deoxy-2-fluoro-β-D-arabinofuranosyl)-9H-purine is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].

  • CAS Number: 109304-04-3
  • MF: C10H12FN5O3
  • MW: 269.23
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 2.0±0.1 g/cm3
  • Boiling Point: 662.9±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 354.7±34.3 °C

5-(2-Hydroxyethyl)uridine

5-(2-Hydroxyethyl)uridine is a thymidine analogue. Analogs of this series have insertional activity towards replicated DNA. They can be used to label cells and track DNA synthesis[1].

  • CAS Number: 102691-28-1
  • MF: C11H16N2O7
  • MW: 288.25
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Malonganenone A

Malonganenone A is a selective plasmodial Hsp70s modulator. It also has antimalarial activity.

  • CAS Number: 882403-69-2
  • MF: C26H38N4O2
  • MW: 438.61
  • Catalog: HSP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3'-O-tert-Butyldimethylsilyl-5'-O-DMT-N2-isobutyrylguanosine 2'-CE phosphoramidite

3'-TBDMS-ibu-rG Phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.

  • CAS Number: 1445905-51-0
  • MF: C50H68N7O9PSi
  • MW: 970.18
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SR31527

SR31527 is a novel allosteric Kinesin-like protein KIFC1 inhibitor that inhibits microtubule-stimulated KIFC1 ATPase activity with IC50 of 6.6 uM, binds directly to KIFC1 with Kd of 25.4 nM; prevents bipolar clustering of extra centrosomes in TNBC cells and significantly reducesTNBC cell colony formation and viability (MDA-MB-231, BT549 and MDA-MB-435s cells IC50=20-30 uM), with less toxicity to normal fibroblasts.

  • CAS Number: 311814-78-5
  • MF: C15H14ClN3OS
  • MW: 319.807
  • Catalog: Kinesin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

LY3143921

LY3143921 (LY-3143921) is an orally available, potent, selective inhibitor of Cdc7 kinase inhibitor, inhibits CDC7/DBF4 I and pMCM2 (S53) with IC50 values of 3.3 nM and 290 nM, respectively. Solid Tumors Phase 1 Clinical

  • CAS Number: 1627696-53-0
  • MF: C16H14FN5O2
  • MW: 327.319
  • Catalog: CDK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2-Aminomethyl adenosine

2-Aminomethyl adenosine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].

  • CAS Number: 2305415-79-4
  • MF: C11H16N6O4
  • MW: 296.28
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3’-Deoxy-3’-fluoro-xylocytidine

3’-Deoxy-3’-fluoro-xylocytidine is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].

  • CAS Number: 26563-01-9
  • MF: C9H12FN3O4
  • MW: 245.21
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.8±0.1 g/cm3
  • Boiling Point: 500.1±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 256.2±32.9 °C

2-(6-amino-8-hydrazinyl-purin-9-yl)-5-(hydroxymethyl)oxolane-3,4-diol

8-Hydrazinoadenosine is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].

  • CAS Number: 3868-34-6
  • MF: C10H15N7O4
  • MW: 297.27
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 2.29g/cm3
  • Boiling Point: 748.8ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 406.7ºC

CFI-402257 hydrochloride

CFI-402257 hydrochloride is a highly selective and orally bioavailable TTK/Mps1 inhibitor with an IC50s of 1.7 nM for TTK in vitro. CFI-402257 hydrochloride has anti-cancer activity[1].

  • CAS Number: 1610677-37-6
  • MF: C28H31ClN6O3
  • MW: 535.04
  • Catalog: Mps1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Deoxythymidine-5'-triphosphate-13C10,15N2 dilithium

Deoxythymidine-5'-triphosphate-13C10,15N2 (dTTP-13C10,15N2) dilithium is 13C and 15N-labeled Deoxythymidine-5'-triphosphate (HY-138615). Deoxythymidine-5'-triphosphate (dTTP) is one of the four nucleoside triphosphates. Deoxythymidine-5'-triphosphate (dTTP) is used in the synthesis of DNA.

  • CAS Number: 2483830-18-6
  • MF: 13C10H15Li215N2O14P3
  • MW: 505.95
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Porfiromycin

Porfiromycin is a bioreductive alkylating agent that preferentially kill hypoxic tumor cells relative to other aerobic counterparts.

  • CAS Number: 801-52-5
  • MF: C16H20N4O5
  • MW: 348.35400
  • Catalog: DNA Alkylator/Crosslinker
  • Density: 1.52g/cm3
  • Boiling Point: 560.9ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 293ºC

1-bromo-2-(2-bromophenyl)disulfanyl-benzene

Tubulin inhibitor 28 (compound 2g) is a potent tubulin inhibitor with an IC50 value of 1.2 µM. Tubulin inhibitor 28 shows anti-proliferative activity for MCF-7 cells[1].

  • CAS Number: 71112-91-9
  • MF: C12H8Br2S2
  • MW: 376.13000
  • Catalog: Microtubule/Tubulin
  • Density: 1.83g/cm3
  • Boiling Point: 386.9ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 187.8ºC

KW-2478

KW-2478 is an inhibitor of Hsp90α, with an IC50 of 3.8 nM, and has antitumor activity against various human hematological tumor cells.

  • CAS Number: 819812-04-9
  • MF: C30H42N2O9
  • MW: 574.662
  • Catalog: HSP
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 746.9±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 405.5±32.9 °C

Cefminox sodium

Cefminox sodium (MT-141) is a semisynthetic cephamycin, which exhibits a broad spectrum of antibacterial activity[1]. Cefminox sodium (MT-141) also acts as a dual agonist of prostacyclin receptor (IP) and PPARγ, upregulates cAMP production and PTEN expression and inhibits Akt/mTOR signaling. Cefminox sodium (MT-141) also prevents pulmonary arterial hypertension[2].

  • CAS Number: 75498-96-3
  • MF: C16H20N7NaO7S3
  • MW: 541.557
  • Catalog: Bacterial
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mertansine

Mertansine (DM1) is a microtubulin inhibitor which binds at the tips of microtubules and suppresses the dynamicity of microtubules.. Mertansine is an antibody-conjugatable maytansinoid that was developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery.

  • CAS Number: 139504-50-0
  • MF: C35H48ClN3O10S
  • MW: 738.288
  • Catalog: Drug-Linker Conjugates for ADC
  • Density: 1.33±0.1 g/cm3
  • Boiling Point: 937.1±65.0 °C at 760 mmHg
  • Melting Point: 190-192 ºC
  • Flash Point: 520.5±34.3 °C

5’-O-DMTr-3’-deoxyuridine

5’-O-DMTr-3’-deoxyuridine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].

  • CAS Number: 86234-42-6
  • MF: C30H30N2O7
  • MW: 530.57
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Marein

Marein has the neuroprotective effect due to a reduction of damage to mitochondria function and activation of the AMPK signal pathway. Marein improves insulin resistance induced by high glucose in HepG2 cells through CaMKK/AMPK/GLUT1 to promote glucose uptake, through IRS/Akt/GSK-3β to increase glycogen synthesis, and through Akt/FoxO1 to decrease gluconeogenesis. Marein is a HDAC inhibitor with an IC50 of 100 µM. Marein has beneficial antioxidative, antihypertensive, antihyperlipidemic and antidiabetic effects[1][2][3].

  • CAS Number: 535-96-6
  • MF: C21H22O11
  • MW: 450.393
  • Catalog: HDAC
  • Density: 1.7±0.1 g/cm3
  • Boiling Point: 835.4±65.0 °C at 760 mmHg
  • Melting Point: 197-202ºC
  • Flash Point: 293.5±27.8 °C

2’-O-Hexadecanyl guanosine

2’-O-Hexadecanyl guanosine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].

  • CAS Number: 2382942-29-0
  • MF: C26H45N5O5
  • MW: 507.67
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

RET-IN-19

RET-IN-19 (compound 59) is a potent RET inhibitor, with IC50 values of 6.8 and 13.51 nM against RET-wt and RET V804M, respectively. RET-IN-19 shows anticancer activity. RET-IN-19 can be used for non-small cell lung cancer (NSCLC) research[1].

  • CAS Number: 2484919-71-1
  • MF: C28H28N6O4S
  • MW: 544.62
  • Catalog: Aurora Kinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Uridine 13C

Uridine 13C is the 13C labeled Uridine[1].

  • CAS Number: 201996-62-5
  • MF: C9H12N2O6
  • MW: 245.19400
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Daunorubicin HCl

Daunorubicin hydrochloride is a topoisomerase II inhibitor with potent antineoplastic activities.

  • CAS Number: 23541-50-6
  • MF: C27H30ClNO10
  • MW: 563.981
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: 770ºC at 760 mmHg
  • Melting Point: 188 - 190ºC
  • Flash Point: 419.5ºC