DNA alkylator/crosslinker is a molecule that alkylates DNA or can cross link with DNA. DNA alkylator/crosslinker can have mutagenic, pharmaceutical, or other effects. Alkylation is the transfer of an alkyl group from one molecule to another. The alkyl group may be transferred as an alkyl carbocation, a free radical, a carbanion or a carbene. Alkylating agents are widely used in chemistry because the alkyl group is probably the most common group encountered in organic molecules. Selective alkylation, or adding parts to the chain with the desired functional groups, is used, especially if there is no commonly available biological precursor. Alkylation with only one carbon is termed methylation. In medicine, alkylation of DNA is used in chemotherapy to damage the DNA of cancer cells. Alkylation is accomplished with the class of drugs called alkylating antineoplastic agents. Crosslinking of DNA occurs when various exogenous or endogenous agents react with two different positions in the DNA. This can either occur in the same strand (intrastrand crosslink) or in the opposite strands of the DNA (interstrand crosslink). Crosslinks also occur between DNA and protein. DNA replication is blocked by crosslinks, which causes replication arrest and cell death if the crosslink is not repaired. The RAD51 family plays a role in repair.


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Temozolomide-d3

Temozolomide-d3 (NSC 362856-d3) is the deuterium labeled Temozolomide. Temozolomide (NSC 362856) is an oral active DNA alkylating agent that crosses the blood-brain barrier. Temozolomide is also a proautophagic and proapoptotic agent. Temozolomide is effective against tumor cells that are characterized by low levels of O6-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system. Temozolomide has antitumor and antiangiogenic effects[1][2].

  • CAS Number: 208107-14-6
  • MF: C6H3D3N6O2
  • MW: 197.16900
  • Catalog: Apoptosis
  • Density: 2.004g/cm3
  • Boiling Point: 526.592ºC at 760 mmHg
  • Melting Point: 202-204ºC
  • Flash Point: 272.273ºC

Cisplatin

Cisplatin is a antineoplastic chemotherapy drug which works by cross-linking with DNA and causing DNA damage in cancer cells.

  • CAS Number: 15663-27-1
  • MF: Cl2H6N2Pt
  • MW: 300.05
  • Catalog: DNA Alkylator/Crosslinker
  • Density: 3.7
  • Boiling Point: N/A
  • Melting Point: 270ºC
  • Flash Point: N/A

WEHI-150

WEHI-150 is a replica of mitoxantrone, is a portent DNA interstrand crosslink[1].

  • CAS Number: 70492-21-6
  • MF: C22H30N6O4
  • MW: 442.51
  • Catalog: DNA Alkylator/Crosslinker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Carboplatin

Carboplatin (NSC 241240) is a DNA synthesis inhibitor which binds to DNA, inhibits replication and transcription and induces cell death. Carboplatin (NSC 241240) is a derivative of cisplatin and a potent anti-cancer agent.

  • CAS Number: 41575-94-4
  • MF: C6H12N2O4Pt
  • MW: 371.254
  • Catalog: Autophagy
  • Density: N/A
  • Boiling Point: 366.4ºCat 760 mmHg
  • Melting Point: 228-230ºC
  • Flash Point: 189.6ºC

Palifosfamide tromethamine

Palifosfamide (tromethamine) is a synthetic alkylating agent with potential antineoplastic activity. As the stabilized active metabolite of ifosfamide, palifosfamide (tromethamine) irreversibly alkylates and crosslinks DNA through GC base pairs. This leads to an inhibition of DNA replication and ultimately cell death. Compared to ifosfamide, palifosfamide (tromethamine) is less toxic.

  • CAS Number: 1070409-31-2
  • MF: C8H22Cl2N3O5P
  • MW: 342.15700
  • Catalog: DNA Alkylator/Crosslinker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Cyclophosphamide-d8

Cyclophosphamide-d8 is deuterium labeled Cyclophosphamide. Cyclophosphamide is a synthetic alkylating agent chemically related to the nitrogen mustards with antineoplastic activity, a immunosuppressant.

  • CAS Number: 1178903-96-2
  • MF: C7H7D8Cl2N2O2P
  • MW: 269.14
  • Catalog: DNA Alkylator/Crosslinker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Duocarmycin analog-2

Duocarmycin analog-2 is a potent DNA alkylating agent. Duocarmycin analog-2 can be used of synthetic immunoconjugate. Duocarmycin analog-2 has antitumor activity[1].

  • CAS Number: 1164275-01-7
  • MF: C29H23ClN4O3
  • MW: 510.97
  • Catalog: DNA Alkylator/Crosslinker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Miriplatin

Miriplatin is a chemotherapy agent which belongs to the class of alkylating agents.

  • CAS Number: 141977-79-9
  • MF: C34H68N2O4Pt
  • MW: 763.999
  • Catalog: DNA Alkylator/Crosslinker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Satraplatin

Satraplatin is an alkylating agent, with potent antitumor effect.

  • CAS Number: 129580-63-8
  • MF: C10H22Cl2N2O4Pt
  • MW: 500.283
  • Catalog: DNA Alkylator/Crosslinker
  • Density: N/A
  • Boiling Point: 134.5ºCat 760 mmHg
  • Melting Point: N/A
  • Flash Point: 32.2ºC

Altretamine

Altretamine is an alkylating antineoplastic agent.

  • CAS Number: 645-05-6
  • MF: C9H18N6
  • MW: 210.279
  • Catalog: DNA Alkylator/Crosslinker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 339.4±25.0 °C at 760 mmHg
  • Melting Point: 171-175 °C(lit.)
  • Flash Point: 159.1±23.2 °C

Illudin M

Illudin M is a cytotoxic fungal sesquiterpene that can be isolated from the culture medium of Omphalotus olearius mushrooms. Illudin M can alkylate DNA. Illudin M has anti-tumor activities[1][2].

  • CAS Number: 1146-04-9
  • MF: C15H20O3
  • MW: 248.31700
  • Catalog: Apoptosis
  • Density: 1.24g/cm3
  • Boiling Point: 452.4ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 241.5ºC

sulfo-DGN462 sodium

sulfo-DGN462 sodium is degraded to DGN462 in culture medium and plasma. DGN462, a potent DNA-alkylating agent, shows anti-tumor activity, such as acute myeloid leukemia (AML)[1].

  • CAS Number: 1401203-09-5
  • MF: C53H60N5NaO12S2
  • MW: 1046.19
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bizelesin

Bizelesin (NSC 615291; U-77779) is an AT-specific DNA alkylating agent that can generate DNA interstrand crosslinks, effectively inhibit DNA replication, and has potential anticancer activity[1].

  • CAS Number: 129655-21-6
  • MF: C43H36Cl2N8O5
  • MW: 815.70300
  • Catalog: DNA Alkylator/Crosslinker
  • Density: 1.604g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tesirine intermediate-2

Tesirine intermediate-2 is the intermediate of Tesirine (HY-128952). Tesirine (SG3249), a pyrrole benzodiazepine (PBD) dimer, is a DNA small channel crosslinker with strong cytotoxicity. Tesirine can be used to synthesize Antibody-Drug Conjugates (ADCs), the warhead component of the payload is SG3199 (HY-101161), which has strong anticancer cell activity.

  • CAS Number: 1430738-34-3
  • MF: C40H55N5O10Si
  • MW: 793.98
  • Catalog: DNA Alkylator/Crosslinker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Semustine

Semustine is a DNA alkylator, binds to DNA, and acts as a cancer chemotherapeutic agent[1].

  • CAS Number: 13909-09-6
  • MF: C10H18ClN3O2
  • MW: 247.72200
  • Catalog: DNA Alkylator/Crosslinker
  • Density: 1.31 g/cm3
  • Boiling Point: N/A
  • Melting Point: 64°C (rough estimate)
  • Flash Point: N/A

RITA (NSC 652287)

RITA is an inhibitor of p53-HDM-2 interaction, binds to p53dN, with a Kd of 1.5 nM, and also induces DNA-DNA cross-links.

  • CAS Number: 213261-59-7
  • MF: C14H12O3S2
  • MW: 292.373
  • Catalog: MDM-2/p53
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 464.9±40.0 °C at 760 mmHg
  • Melting Point: 160 °C
  • Flash Point: 235.0±27.3 °C

Duocarmycin

Duocarmycin is based on its characteristic curved indole structure and a spirocyclopropylcyclohexadienone electrophile to act anticancer activity. Duocarmycin is a DNA minor groove binding alkylating agent and explored as drug–antibody conjugates (ADCs) [1].

  • CAS Number: 1116745-06-2
  • MF: C26H26ClN3O3
  • MW: 463.96
  • Catalog: DNA Alkylator/Crosslinker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

melphalan

Melphalan is an effective DNA alkylating agent, with potent antitumor activity.

  • CAS Number: 148-82-3
  • MF: C13H18Cl2N2O2
  • MW: 305.200
  • Catalog: DNA Alkylator/Crosslinker
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 473.1±45.0 °C at 760 mmHg
  • Melting Point: ~180 °C
  • Flash Point: 239.9±28.7 °C

[2-(11,17-dihydroxy-10,13-dimethyl-3-oxo-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-17-yl)-2-oxo-ethyl] 4-[4-[bis(2-chloroethyl)amino]phenyl]butanoate

Prednimustine (Leo 1031;NSC 134087) is the ester formed from Prednisolone (HY-17463) and Chlorambucil (HY-13593). Prednimustine can be used for leukemias and lymphomas research[1].

  • CAS Number: 29069-24-7
  • MF: C35H45Cl2NO6
  • MW: 646.64100
  • Catalog: DNA Alkylator/Crosslinker
  • Density: 1.3g/cm3
  • Boiling Point: 791.5ºC at 760 mmHg
  • Melting Point: 163-164ºC
  • Flash Point: 432.5ºC

Temozolomide

Temozolomide (NSC 362856; CCRG 81045) is an oral DNA alkylating agent used to treat some brain cancers.

  • CAS Number: 85622-93-1
  • MF: C6H6N6O2
  • MW: 194.151
  • Catalog: Autophagy
  • Density: 2.0±0.1 g/cm3
  • Boiling Point: 526.6±42.0 °C at 760 mmHg
  • Melting Point: 212°C dec.
  • Flash Point: 272.3±27.9 °C

Palifosfamide

Palifosfamide is a novel DNA alkylator and the active metabolite of ifosfamide, with antitumor activity.

  • CAS Number: 31645-39-3
  • MF: C4H11Cl2N2O2P
  • MW: 221.022
  • Catalog: DNA Alkylator/Crosslinker
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 341.5±52.0 °C at 760 mmHg
  • Melting Point: 106-107ºC
  • Flash Point: 160.4±30.7 °C

Fotemustine

Fotemustine is a DNA-alkylating agent, with antitumor activity.

  • CAS Number: 92118-27-9
  • MF: C9H19ClN3O5P
  • MW: 315.691
  • Catalog: DNA Alkylator/Crosslinker
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 188 °C(lit.)
  • Melting Point: 85ºC
  • Flash Point: 104 °F

Lomustine

Lomustine is a DNA alkylating agent, with antitumor activity.

  • CAS Number: 13010-47-4
  • MF: C9H16ClN3O2
  • MW: 233.695
  • Catalog: Autophagy
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: 88-90
  • Flash Point: N/A

3-Pyrrolidinone,5-[[[(1,1-dimethylethyl)dimethylsilyl]oxy]methyl]-1-[5-methoxy-2-nitro-4-[[tris(1-methylethyl)silyl]oxy]benzoyl]-,(5S)-

Tesirine intermediate-1 is the intermediate of Tesirine (HY-128952). Tesirine (SG3249), a pyrrole benzodiazepine (PBD) dimer, is a DNA small channel crosslinker with strong cytotoxicity. Tesirine can be used to synthesize Antibody-Drug Conjugates (ADCs), the warhead component of the payload is SG3199 (HY-101161), which has strong anticancer cell activity.

  • CAS Number: 1430738-05-8
  • MF: C28H48N2O7Si2
  • MW: 580.86
  • Catalog: DNA Alkylator/Crosslinker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

EC2629

EC2629 is a highly potent folate receptor (FR)-targeted DNA crosslinking agent. EC2629 can be used for the research of FR-positive tumors, including those that are classified as drug resistant[1].

  • CAS Number: 2245361-43-5
  • MF: C103H138N24O35S3
  • MW: 2368.53
  • Catalog: DNA Alkylator/Crosslinker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

KCC 07

KCC-07 is a potent, selective and brain-penetrant MBD2 (methyl-CpG-binding domain protein 2) inhibitor. KCC-07 prevents binding of MBD2 to methylated DNA and activates brain specific angiogenesis inhibitor 1 (BAI1) inducing anti-proliferative BAI1/p53/p21 signaling. Anticancer activity[1].

  • CAS Number: 315702-75-1
  • MF: C14H11N3OS
  • MW: 269.32
  • Catalog: DNA Alkylator/Crosslinker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bendamustine-d8

Bendamustine-d8 is the deuterium labeled Bendamustine[1]. Bendamustine (SDX-105 free base), a purine analogue, is a DNA cross-linking agent. Bendamustine activates DNA-damage stress response and apoptosis. Bendamustine has potent alkylating, anticancer and antimetabolite properties[2].

  • CAS Number: 1134803-33-0
  • MF: C16H13D8Cl2N3O2
  • MW: 366.312
  • Catalog: Apoptosis
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 585.2±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 307.7±30.1 °C

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

Bendamustine Hydrochloride

Bendamustine hydrochloride is a DNA cross-linking agent that causes DNA breaks, with alkylating and antimetabolite properties.

  • CAS Number: 3543-75-7
  • MF: C16H22Cl3N3O2
  • MW: 394.724
  • Catalog: DNA Alkylator/Crosslinker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: 149-151°C
  • Flash Point: N/A

4-Hydroperoxy cyclophosphamide

4-Hydroperoxy cyclophosphamide is the active metabolite form of the prodrug Cyclophosphamide. 4-Hydroperoxy cyclophosphamide crosslinks DNA and induces T cell apoptosis independent of death receptor activation, but activates mitochondrial death pathways through production of reactive oxygen species (ROS). 4-Hydroperoxy cyclophosphamide is used to treat lymphomas and autoimmune disorders.

  • CAS Number: 39800-16-3
  • MF: C7H15Cl2N2O4P
  • MW: 293.08500
  • Catalog: Apoptosis
  • Density: 1.465g/cm3
  • Boiling Point: 419.946ºC at 760 mmHg
  • Melting Point: 100-103ºC
  • Flash Point: 207.776ºC