DNA Alkylator/Crosslinker(DNA烷化剂/交联剂)
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.
Products for DNA Alkylator/Crosslinker
- Cat.No. 产品名称 Information
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GC61182
Phosphoramide mustard (cyclohexanamine)
NSC 69945, PMC
An alkylating agent and active metabolite of cyclophosphamide -
GC61188
PIP-199
PIP-199是一种RecQ介导的基因组不稳定蛋白RMI核心复合物/MM2相互作用(RMIcorecomplex/MM2interaction)的选择性抑制剂,其IC50值为36μM。MM2是FANCM上RMI复合物的结合位点。PIP-199可用于耐受肿瘤对DNA交联化疗药物的增敏研究。
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GC32946
PK11007
PK11000 stabilizes the DBD of both WT and mutant p53 proteins by covalent cysteine modification without compromising DNA binding and effective in inducing cell death.
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GC63154
PR-104
PR-104 是一种选择性缺氧激活的 DNA 交联剂,可用于多种异种肿瘤模型的研究。PR-104 作为氮芥的前体药物,可有效地转化为亲脂性较强的二硝基苯甲酰胺芥菜醇 PR-104A。
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GC62490
PR-104A
SN 27858
PR-104A (SN 27858) 是磷酸盐前药 PR-104 的醇代谢物。PR-104A 是一种缺氧选择性的 DNA 交联剂/DNA 损伤剂,也是一种细胞毒素。具有抗肿瘤活性。PR-104A 在缺氧条件下通过 1-电子 NADPH:细胞色素 P450 氧化还原酶代谢。可用于复发/难治性 T 系急性淋巴细胞白血病 (T-ALL) 的研究。 -
GC11793
Procarbazine HCl
盐酸甲基苄肼
A DNA methylating agent -
GC12793
RITA (NSC 652287)
5,5'-(2,5-呋喃二基)二-2-噻吩甲醇,NSC 652287
An inhibitor of the p53-HDM-2 interaction -
GC37593
Satraplatin
沙铂; BMS182751; BMY45594; JM216
An orally available antineoplastic platinum(IV) complex -
GC38349
Seco-Duocarmycin SA
Seco-Duocarmycin SA 是一种高效的 DNA 烷化剂 (DNA alkylator),可作用做抗体-药物偶联物 (ADC) 的毒素部分。
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GC38354
Seco-Duocarmycin TM
Seco-Duocarmycin TM 是 Duocarmycins 家族的一种 DNA 烷化剂,可抑制 DNA 合成。Seco-Duocarmycin TM 是一种细胞毒性剂,用作抗体-药物偶联物中的细胞毒性成分。
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GC37625
Semustine
司莫司汀
Semustine 是一种 DNA 烷化剂,与 DNA 结合,作为癌症化疗剂。 -
GC69882
SG2057
DRG16
SG2057 (DRG16) 是一种含有戊二氧基键的 PBD 二聚体,该键选择性地结合 DNA 小沟中的序列,形成 DNA 链间和链内交联加合物。SG2057 是一种高效抗肿瘤剂。 -
GC62691
SG3199
SG3199 是一种具有细胞毒性的 DNA 小沟链间交联 PDB 二聚体。SG3199 是 ADC 有效载荷 Tesirine (SG3249) 的组成成分。
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GC34086
SJG-136 (NSC-694501)
NSC-694501
SJG-136 (NSC-694501) 是一种 DNA 交联剂,对于 pBR322 DNA 的 XL50 为 45 nM。 SJG-136 (NSC-694501) 具有有效的抗肿瘤活性。 -
GC17131
Streptozocin
链脲佐菌素; Streptozotocin; U 9889
Streptozocin 是一种有效的 DNA 甲基化抗生素,是一种天然存在的亚硝基酰胺,在实验模型中广泛用于产生糖尿病。 -
GC13667
Temozolomide
替莫唑胺; NSC 362856; CCRG 81045; TMZ
替莫唑胺是一种口服活性烷化剂,可诱导 DNA 中 O6-甲基鸟嘌呤的形成,其在随后的 DNA 复制周期中与胸腺嘧啶错配,从而激活细胞凋亡途径,替莫唑胺可穿过血脑屏障并适用于恶性神经胶质瘤和转移性黑色素瘤。 -
GC52076
Temozolomide Acid
3,4-二氢-3-甲基-4-氧代咪唑并[5,1-D]-1,2,3,5-四嗪-8-甲酰胺酸
An active metabolite of temozolomide -
GC74145
Tesirine intermediate-1
Tesirine intermediate-1是Tesirine的中间体。
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GC74107
Tesirine intermediate-2
Tesirine intermediate-2是Tesirine的中间体。
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GC16158
Thio-TEPA
三亚乙基硫代磷酰胺
An alkylating agent with anticancer activity -
GC32918
Treosulfan (NSC 39069)
曲奥舒凡,NSC 39069; Treosulphan
Treosulfan (NSC 39069, Treosulphan) is an alkylating agent used for conventional and high-dose chemotherapy regimens. Treosulfan is potently cytotoxic against pancreatic cancer cell lines. -
GC37860
Uramustine
Uramustine 是一种可口服的烷化剂 (alkylator),可用于治疗淋巴肉瘤、慢性淋巴性白血病和血小板增多症。
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GC10339
VAL-083
去水卫矛醇; Dianhydrodulcitol; Dianhydrogalactitol
VAL-083 是一种烷化剂,可在 DNA 上产生 N7 甲基化,具有抗肿瘤活性。