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Imatinib inhibits the SLF-dependent activation of wild-type c-kit kinase activity with an IC50 for these effects of approximately 0.1 μM, which is similar to the concentration required for inhibition of PDGFR. Imatinib is an oral chemotherapy agent used to treat cancers. Specifically, it is used for chronic myelogenous leukemia (CML) and acute lymphocytic leukemia (ALL) that are Philadelphia chromosome-positive (Ph+), certain types of gastrointestinal stromal tumors (GIST), hypereosinophilic syndrome (HES), chronic eosinophilic leukemia (CEL), systemic mastocytosis, and myelodysplastic syndrome. Synonyms: CGP057148B; STI571; Gleevec; Glivec; N-(4-Methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)-4-((4-methylpiperazin-1-yl)methyl)benzamide; 4-[(4-Methyl-1-piperazinyl)methyl]-N-(4-methyl-3-{[4-(3-pyridinyl)-2-pyrimidinyl]amino}phenyl)benzamide. Grade: >98%. CAS No. 152459-95-5. Molecular formula: C29H31N7O. Mole weight: 493.60.
Imatinib
Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL , v-Abl , PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively [1] [2] [3] [4]. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV [5]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: STI571; CGP-57148B. CAS No. 152459-95-5. Pack Sizes: 10 mM * 1 mL; 200 mg; 500 mg; 1 g; 5 g. Product ID: HY-15463.
Imatinib-[d3]
Imatinib-[d3] is the labelled analogue of Imatinib. Imatinib can be used for the treatment of chronic myelogenous leukemia and acute lymphocytic leukemia. Synonyms: Imatinib D3; Genfatinib-d3; 4-[[4-(methyl-d3)-1-piperazinyl]methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]benzamide. Grade: 95% by HPLC; 99% atom D. CAS No. 1134803-18-1. Molecular formula: C29H28D3N7O. Mole weight: 496.62.
Imatinib-D3
Imatinib-D3. Uses: For analytical and research use. Group: Impurity standards. CAS No. 1134803-18-1. Molecular formula: C29H28D3N7O. Mole weight: 496.63. Catalog: APB1134803181.
Imatinib-[d4]
Imatinib-[d4] is an isotopically labelled analogue of Imatinib. Imatinib is an inhibitor of multiple tyrosine kinases. It is a COVID-19-related research product. Synonyms: N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)-4-((4-methylpiperazin-1-yl)methyl)benzamide-2,3,5,6-d4; Imatinib D4. Grade: ≥98% (HPLC). CAS No. 1134803-16-9. Molecular formula: C29H27D4N7O. Mole weight: 497.64.
Imatinib-D4
Imatinib-D4. Uses: For analytical and research use. Group: Impurity standards. CAS No. 1134803-16-9. Molecular formula: C29H27D4N7O. Mole weight: 497.64. Catalog: APB1134803169.
Imatinib-d8
Imatinib-d8 is a deuterated tyrosine kinase inhibitor. Group: Biochemicals. Grades: Highly Purified. CAS No. 1092942-82-9. Pack Sizes: 1mg, 10mg. Molecular Formula: C29H23D8N7O. US Biological Life Sciences.
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Imatinib-[d8]
Imatinib-[d8] is the labelled analogue of Imatinib, a treatment of chronic myeloid leukemia. Synonyms: Imatinib D8; 4-[(4-Methyl-1-piperazinyl-2,2,3,3,5,5,6,6-d8)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]benzamide; Genfatinib-d8. Grade: 95% by HPLC; 95% atom D. CAS No. 1092942-82-9. Molecular formula: C29H23D8N7O. Mole weight: 501.65.
A deuterated tyrosine kinase inhibitor. Highly specific for BCR-ABL, the enzyme associated with chronic myelogenous leukemia (CML) and certain forms of acute lymphoblastic leukemia (ALL). Group: Biochemicals. Alternative Names: Imatinib-d8 Methanesulfonate, STI-571-d8, CGP-57148B-d8, Glivec-d8. Grades: Highly Purified. Pack Sizes: 500ug. US Biological Life Sciences.
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Imatinib free base
Imatinib is a tyrosine kinase inhibitor with antineoplastic activity. Imatinib binds to an intracellular pocket located within tyrosine kinases (TK), thereby inhibiting ATP binding and preventing phosphorylation and the subsequent activation of growth receptors and their downstream signal transduction pathways. This agent inhibits TK encoded by the bcr-abl oncogene as well as receptor TKs encoded by the c-kit and platelet-derived growth factor receptor (PDGFR) oncogenes. Imatinib was approved for medical use in the United States in 2001. Uses: Designed for use in research and industrial production. Additional or Alternative Names: CGP 57148; CGP57148; CGP-57148; CGP57148B; CGP-57148B; CGP 57148B; STI571; STI-571; STI 571. Product Category: Inhibitors. Appearance: White to off-white to brownish or yellowish tinged crystalline powder. CAS No. 152459-95-5. Molecular formula: C29H31N7O. Mole weight: 493.62. Purity: >98%. IUPACName: N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)-4-((4-methylpiperazin-1-yl)methyl)benzamide. Canonical SMILES: O=C(NC1=CC=C(C)C(NC2=NC=CC(C3=CC=CN=C3)=N2)=C1)C4=CC=C(CN5CCN(C)CC5)C=C4. Product ID: ACM152459955. Alfa Chemistry ISO 9001:2015 Certified.
Imatinib, Free base
An inhibitor of the bcr-abl tyrosine kinase. It acts by binding to the ATP binding site of bcr-abl. Imatinib also stimulates the entry of the bcr-abl tyrosine kinase into the nucleus, where it cannot perform its anti-apoptopic functions. It inhibits EOL-1 cell viability (IC50=0.5nm), phosphorylation of a fusion protein (IC50=30nm), and viability of BaF3 cells expressing Rhe-PDGFRa in the absence of IL-3 (IC50 =0.17nm). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 100ug, 1g. US Biological Life Sciences.
Worldwide
Imatinib Imidazole Impurity
Imatinib Imidazole Impurity. Uses: For analytical and research use. Group: Impurity standards. CAS No. 1256080-10-0. Molecular formula: C32H31N9O2. Mole weight: 573.66. Catalog: APB1256080100.
Imatinib Impurity 12
Imatinib Impurity 12. Uses: For analytical and research use. Group: Impurity standards. CAS No. 112696-91-0. Molecular formula: C16H15N5. Mole weight: 277.33. Catalog: APB112696910.
Imatinib Impurity 16
Imatinib Impurity 16. Uses: For analytical and research use. Group: Impurity standards. CAS No. 152460-09-8. Molecular formula: C16H13N5O2. Mole weight: 307.31. Catalog: APB152460098.
Imatinib Impurity 3
Imatinib Impurity 3. Uses: For analytical and research use. Group: Impurity standards. CAS No. 152459-96-6. Molecular formula: C24H21N5O. Mole weight: 395.47. Catalog: APB152459966.
Imatinib Impurity 36
Imatinib Impurity 36. Uses: For analytical and research use. Group: Impurity standards. CAS No. 106261-48-7. Molecular formula: C13H18N2O2. Mole weight: 234.3. Catalog: APB106261487.
Imatinib Impurity 5
Imatinib Impurity 5. Uses: For analytical and research use. Group: Impurity standards. CAS No. 1032314-73-0. Molecular formula: C17H17N5. Mole weight: 291.36. Catalog: APB1032314730.
Imatinib Impurity 8
Imatinib Impurity 8. Uses: For analytical and research use. Group: Impurity standards. CAS No. 1407229-73-5. Molecular formula: C21H25N2O4+. Mole weight: 369.44. Catalog: APB1407229735.
Imatinib impurity D
Imatinib impurity D. Uses: For analytical and research use. Group: Impurity standards. Alternative Names: 6-methyl-N1-(4-(pyridin-3-yl)pyrimidin-2-yl)benzene-1,3-diamine. CAS No. 152460-10-1. Molecular formula: C16H15N5. Mole weight: 277.32. Catalog: APB152460101.
Imatinib impurity J
Imatinib impurity J. Uses: For analytical and research use. Group: Impurity standards. Alternative Names: (E)-3-(dimethylamino)-1-(pyridin-3-yl)prop-2-en-1-one. CAS No. 123367-26-0. Molecular formula: C10H12N2O. Mole weight: 176.22. Catalog: APB123367260.
Imatinib Intermediate 1
Imatinib Intermediate 1. Uses: For analytical and research use. Group: Impurity standards. CAS No. 125743-63-7. Molecular formula: C13H17N3. Mole weight: 215.3. Catalog: APB125743637.
Imatinib Intermediate 2
Imatinib Intermediate 2. Uses: For analytical and research use. Group: Impurity standards. CAS No. 106261-49-8. Molecular formula: C13H20Cl2N2O2. Mole weight: 307.22. Catalog: APB106261498.
Imatinib Intermediate 3
Imatinib Intermediate 3. Uses: For analytical and research use. Group: Impurity standards. CAS No. 1407124-83-7. Molecular formula: C16H13N5O. Mole weight: 291.31. Catalog: APB1407124837.
Imatinib Intermediate 5
Imatinib Intermediate 5. Uses: For analytical and research use. Group: Impurity standards. CAS No. 106261-64-7. Molecular formula: C13H19Cl3N2O. Mole weight: 325.66. Catalog: APB106261647.
Imatinib mesylate
100mg Pack Size. Group: Bioactive Small Molecules, Research Organics & Inorganics. Formula: C29H31N7O · CH4O3S. CAS No. 220127-57-1. Prepack ID 60579435-100mg. Molecular Weight 589.71. See USA prepack pricing.
Imatinib mesylate
Imatinib (INN), marketed by Novartis as Gleevec (Canada, South Africa and the USA) or Glivec (Australia, Europe and Latin America), and sometimes referred to by its investigational name STI-571, is a tyrosine-kinase inhibitor used in the treatment of multiple cancers, most notably Philadelphia chromosome-positive (Ph+) chronic myelogenous leukemia (CML). Synonyms: CGP-57148B; CGP 57148B; CGP57148B; Gleevec, Imatinib. Grade: >98%. CAS No. 220127-57-1. Molecular formula: C29H31N7O.CH4SO3. Mole weight: 589.71.
Imatinib Mesylate
Imatinib Mesylate (STI571 Mesylate) is a tyrosine kinases inhibitor that inhibits c-Kit , Bcr-Abl , and PDGFR ( IC 50 =100 nM) tyrosine kinases. Uses: Scientific research. Group: Signaling pathways. Alternative Names: STI571 Mesylate; CGP-57148B Mesylate. CAS No. 220127-57-1. Pack Sizes: 10 mM * 1 mL; 200 mg; 500 mg; 1 g; 5 g. Product ID: HY-50946.
Imatinib Meta-methyl-piperazine Impurity
Imatinib impurity. Group: Biochemicals. Alternative Names: 3- [ (4-Methyl-1-piperazinyl) methyl] -N- [4-methyl-3- [ (4-pyridinyl) -2-pyrimidinylamino] phenyl] benzamide. Grades: Highly Purified. CAS No. 1246819-59-9. Pack Sizes: 25mg. US Biological Life Sciences.
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Imatinib, Methanesulfonate Salt (STI-571, CGP-57148B)
A tyrosine kinase inhibitor. Highly specific for BCR-ABL, the enzyme associated with chronic myelogenous leukemia (CML) and certain forms of acute lymphoblastic leukemia (ALL). Imatinib inhibits bcr-abl tyrosine kinase activity, upon which some types of tumor cells depend for growth. Imatinib acts by binding to the ATP binding site of bcr-abl and competitively inhibiting its tyrosine kinase activity. Imatinib is selective for bcr-abl, but it also targets several other kinases (c-kit and PDGF-R). (1). Group: Biochemicals. Alternative Names: 4- [ (4-Methyl-1-piperazinyl) methyl] -N- [4-methyl-3- [ [4- (3-pyridinyl) -2-pyrimidinyl] amino] phenyl] benzamide Methanesulfonate; CGP 57148B; Imatinib Mesilate; Imatinib Methanesulfonate; Imatinib Mesylate; STI 571; Bcr-abl Inhibitor IV; Abl Inhibitor V, PDGFR Tyrosine Kinase Inhibitor XXIV, c-Kit Inhibitor IV. Grades: Highly Purified. CAS No. 220127-57-1. Pack Sizes: 25mg, 1g, 5g, 10g. US Biological Life Sciences.
Worldwide
Imatinib Para-Diamino Methyl Benzene
Imatinib Para-Diamino Methyl Benzene. Uses: For analytical and research use. Group: Impurity standards. CAS No. 1026753-54-7. Molecular formula: C29H31N7O. Mole weight: 493.61. Catalog: APB1026753547.
Imatinib Para-diaminomethylbenzene Impurity Hydrochloride Salt
Imatinib Para-diaminomethylbenzene Impurity Hydrochloride Salt. Uses: For analytical and research use. Group: Impurity standards. Catalog: APS001961. Format: Neat.
Des(methylpiperazinyl-N-methyl) Imatinib Dimer Impurity. Uses: For analytical and research use. Group: Impurity standards. CAS No. 1365802-18-1. IUPAC Name: N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]-4-[[4-[[4-[[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]carbamoyl]phenyl]methyl]piperazin-1-yl]methyl]benzamide. Molecular formula: C52H48N12O2. Mole weight: 873.02. Catalog: APS1365802181. SMILES: Cc1ccc(NC(=O)c2ccc(CN3CCN(Cc4ccc(cc4)C(=O)Nc5ccc(C)c(Nc6nccc(n6)c7cccnc7)c5)CC3)cc2)cc1Nc8nccc(n8)c9cccnc9. Format: Neat.
N-Boc-N-Desmethyl Imatinib
Imatinib derivative. Group: Biochemicals. Alternative Names: 4- [ [4- [ [ [4-Methyl-3- [ [4- (3-pyridinyl) -2-pyrimidinyl] amino] phenyl] amino] carbonyl] phenyl] methyl] -1-piperazinecarboxylic Acid 1,1-Dimethylethyl Ester. Grades: Highly Purified. CAS No. 1076199-23-9. Pack Sizes: 1mg. US Biological Life Sciences.
Worldwide
N-Boc-N-Desmethyl Imatinib (Piperidine)-1-oxide
N-Boc-N-Desmethyl Imatinib (Piperidine)-1-oxide. Uses: For analytical and research use. Group: Impurity standards. Catalog: APS002480. Format: Neat.
N-Desmethyl imatinib
N-Desmethyl imatinib. Group: Biochemicals. Alternative Names: N- [4-Methyl-3- [ [4- (3-pyridinyl) -2-pyrimidinyl] amino] phenyl] -4- (1-piperazinylmethyl) -benzamide; N-Desmethyl gleevec; CGP-74588. Grades: Highly Purified. CAS No. 404844-02-6. Pack Sizes: 1mg, 2mg, 5mg. Molecular Formula: C28H29N7O. US Biological Life Sciences.
Worldwide
N-Desmethyl imatinib
N-Desmethyl imatinib (Norimatinib) is a metabolite of Imatinib (HY-15463). Imatinib is a multi-target inhibitor of v-Abl, c-Kit and PDGFR [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: Norimatinib; Imatinib metabolite N-Desmethyl imatinib. CAS No. 404844-02-6. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 50 mg. Product ID: HY-G0017.
N-Desmethyl Imatinib (CGP-74588)
A metabolite of Imatinib, a tyrosine kinase inhibitor which is highly specific for BCR-ABL, the enzyme associated with chronic myelogenous leukemia (CML) and certain forms of acute lymphoblastic leukemia (ALL). Group: Biochemicals. Alternative Names: N-Desmethyl Gleevec, CGP-74588. Grades: Highly Purified. CAS No. 404844-02-6. Pack Sizes: 500ug. US Biological Life Sciences.
Worldwide
N-Desmethyl Imatinib-[d4]
N-Desmethyl Imatinib-[d4] is the labelled analogue of N-Desmethyl Imatinib, which is a metabolite of Imatinib. Synonyms: Desmethyl imatinib D4; N-Desmethyl Imatinib-d4; N-[4-Methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-4-(1-piperazinylmethyl)-benzamide-d4; N-Desmethyl Gleevec-d4; Norimatinib-d4; Imatinib EP Impurity C-d4. Grade: 95% by HPLC; 98% atom D. Molecular formula: C28H25D4N7O. Mole weight: 483.60.
N-Desmethyl Imatinib-d8
A deuterated metabolite of N-Desmethyl Imatinib, a tyrosine kinase inhibitor which is highly specific for BCR-ABL, the enzyme associated with chronic myelogenous leukemia (CML) and certain forms of acute lymphoblastic leukemia (ALL). Group: Biochemicals. Alternative Names: N-Desmethyl Gleevec-d8. Grades: Highly Purified. Pack Sizes: 250ug. US Biological Life Sciences.
Worldwide
N-Desmethyl Imatinib-[d8]
N-Desmethyl Imatinib-[d8] is a deuterated metabolite of gleevec, a tyrosine kinase inhibitor specific for BCR-ABL, the enzyme associated with chronic myelogenous leukemia (CML) and certain forms of acute lymphoblastic leukemia (ALL). Synonyms: N-Desmethyl Imatinib D8; N-Desmethyl Gleevec-d8. Grade: ≥96% by HPLC; ≥98% atom D. CAS No. 1185103-28-9. Molecular formula: C28H21D8N7O. Mole weight: 487.64.
N-Desmethyl Imatinib (Piperidine)-1-oxide Hydrochloride. Uses: For analytical and research use. Group: Impurity standards. Catalog: APS002500. Format: Neat.
17-AAG hydrochloride
17-AAG hydrochloride is a potent HSP90 inhibitor with IC50 value of 5 nM, which is a 100-fold higher binding affinity for HSP90 derived from tumour cells than that from normal cells. It is less toxic by binding to Hsp90 and altering its function. It causes the degradation of HER2, HER3, Akt, and both mutant and wild-type androgen receptor (AR), leading to the RB-dependent G1 growth arrest of prostate cancer cells. It has the ability to induce apoptosis of cells transformed with imatinib mesylate-resistant T315I and E255K BCR-ABL mutants with IC50 values of 2.3 μM and 1.0 μM, respectively. It displays significantly higher binding affinity for Hsp90 from 3T3-src, B16 or CT26 xenografts in nude mice compared with that from the normal tissues in vivo. Uses: 17-aag hydrochloride has the ability to induce apoptosis of cells transformed with imatinib mesylate-resistant t315i and e255k bcr-abl mutants. Synonyms: 17-AAG hydrochloride; 17 AAG hydrochloride; 17AAG hydrochloride; [(3R,5S,6R,7S,8E,10S,11S,12Z,14E)-6-hydroxy-5,11-dimethoxy-3,7,9,15-tetramethyl-16,20,22-trioxo-21-(prop-2-enylamino)-17-azabicyclo[16.3.1]docosa-1(21),8,12,14,18-pentaen-10-yl] carbamate hydrochloride; Tanespimycin Hydrochloride; NSC 330507 Hydrochloride; CP 127374 Hydrochloride; 17-(Allylamino)-17-desmethylgeldanamycin hydrochloride. Grade: >98%. CAS No. 911710-03-7. Molecular formula: C31H44ClN3O8. Mole weight: 622.15.
1-Methyl-1,4-bis[[4-[[[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]amino]carbonyl]phenyl]methyl]-piperazinium. Uses: For analytical and research use. Group: Impurity standards. Alternative Names: Des(methylpiperazinyl) Imatinib Dimer Piperazinium Chloride,Piperazinium, 1-methyl-1,4-bis[[4-[[[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]amino]carbonyl]phenyl]methyl]-. CAS No. 1821122-73-9. IUPAC Name: 4-[[4-methyl-4-[[4-[[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]carbamoyl]phenyl]methyl]piperazin-4-ium-1-yl]methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide. Molecular formula: C53H51N12O2. Mole weight: 888.05. Catalog: APS1821122739. SMILES: Cc1ccc(NC(=O)c2ccc(CN3CC[N+](C)(Cc4ccc(cc4)C(=O)Nc5ccc(C)c(Nc6nccc(n6)c7cccnc7)c5)CC3)cc2)cc1Nc8nccc(n8)c9cccnc9. Format: Neat.
2-((4-Methylpiperazin-1-yl)methyl)benzonitrile
2-((4-Methylpiperazin-1-yl)methyl)benzonitrile is an impurity of Imatinib (G407000). Group: Biochemicals. Grades: Highly Purified. CAS No. 864069-00-1. Pack Sizes: 500mg, 1g. Molecular Formula: C13H17N3, Molecular Weight: 215.29. US Biological Life Sciences.
Worldwide
2-Methyl-5-nitroaniline
2-Methyl-5-nitroaniline is used as a reagent in the synthesis of imatinib base derivatives which show antibacterial and antifungal activity. Also used as a reagent in the synthesis of pyrimidinylamino Benzene derivatives which exhibit antiproliferative activity against melanoma. Group: Biochemicals. Grades: Highly Purified. CAS No. 99-55-8. Pack Sizes: 1g, 10g. Molecular Formula: C7H8N2O2, Molecular Weight: 152.15. US Biological Life Sciences.
Worldwide
3-Acetylpyridine
3-Acetylpyridine. Uses: For analytical and research use. Group: Impurity standards. Alternative Names: Imatinib Mesilate Imp. H (EP), 1-(Pyridin-3-yl)ethan-1-one, 3-Acetylpyridine. CAS No. 350-03-8. IUPAC Name: 1-pyridin-3-ylethanone. Molecular formula: C7H7NO. Mole weight: 121.14. Catalog: APS350038. SMILES: CC(=O)c1cccnc1. Format: Neat.
4-(4-Methyl-1-piperazinylmethyl)benzoic Acid
An Intermediate of Imatinib. Synonyms: 4-[(4-methyl-1-piperazinyl)methyl]benzoic acid; 4-[(4-methylpiperazin-1-yl)methyl]benzoic acid. Grade: > 95 %. CAS No. 106261-48-7. Molecular formula: C13H18N2O2. Mole weight: 234.29.
5-(5-Fluoro-2-oxo-1,2-dihydro-indol-3-ylidenemethyl)-2,4-dimethyl-1H-pyrrole-3-carboxylic Acid is an intermediate of. Sunitinib, which is an oral, small-molecule, multi-targeted receptor tyrosine kinase (RTK) inhibitor for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST). Uses: Sunitinib intermediate. Synonyms: 5-[(5-Fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxylic acid; 1H-Pyrrole-3-carboxylic acid, 5-[(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-. Grade: ≥95%. CAS No. 452105-33-8. Molecular formula: C16H13FN2O3. Mole weight: 300.29.
5-Fluoro-2-oxindole
5-Fluoro-2-oxindole is an impurity of Sunitinib, which is an oral, small-molecule, multi-targeted receptor tyrosine kinase (RTK) inhibitor for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST). Synonyms: 2H-Indol-2-one, 5-fluoro-1,3-dihydro-; 5-Fluoro-1,3-dihydro-2H-indol-2-one; 5-Fluoro-2,3-dihydro-2-oxoindole; 5-Fluoro-2,3-dihydroindol-2-one; 5-Fluoro-2-oxoindoline; 5-Fluoroindolin-2-one; 5-Fluorooxindole. Grade: ≥95%. CAS No. 56341-41-4. Molecular formula: C8H6FNO. Mole weight: 151.14.
5-Formyl-2,4-dimethyl-1H-pyrrole-3-carboxylic acid is an impurity of Sunitinib, which is an oral, small-molecule, multi-targeted receptor tyrosine kinase (RTK) inhibitor for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST). Synonyms: 1H-Pyrrole-3-carboxylic acid, 5-formyl-2,4-dimethyl-; 2,4-Dimethyl-5-formyl-1H-pyrrole-3-carboxylic acid; 2,4-Dimethyl-5-formylpyrrole-3-carboxylic acid; 5-Formyl-2,4-dimethylpyrrole-3-carboxylic acid. Grade: ≥95%. CAS No. 253870-02-9. Molecular formula: C8H9NO3. Mole weight: 167.16.
Bafetinib
A substituted benzamide derivative structurally related to STI-571 (Imatinib Mesylate). It was identified as highly potent Bcr-Abl kinase inhibitor. Group: Biochemicals. Alternative Names: N-[3- ([4, 5'-Bipyrimidin]-2-ylamino) -4-methylphenyl]-4-[[ (3S) -3- (dimethylamino) -1-pyrrolidinyl]methyl]-3- (trifluoromethyl) benzamide; INNO 406; NS 187. Grades: Highly Purified. CAS No. 859212-16-1. Pack Sizes: 1mg. US Biological Life Sciences.
Worldwide
Bosutinib monohydrate
Bosutinib hydrate is a Src/Abl inhibitor used in the treatment of chronic myeloid leukemia (CML), a type of cancer that affects the blood and bone marrow. Bosutinib is a tyrosine kinase inhibitor that works by blocking the activity of BCR-ABL, a protein that promotes the growth of abnormal leukemia cells in patients with CML. BCR-ABL is formed as a result of a genetic abnormality known as the Philadelphia chromosome. It is indicated for the treatment of adults with newly diagnosed chronic phase CML as well as CML that is resistant or intolerant to prior therapy, including imatinib. Synonyms: Bosutinib hydrate; 3-Quinolinecarbonitrile, 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-piperazinyl)propoxy]-, hydrate (1:1); 4-[(2,4-Dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-piperazinyl)propoxy]-3-quinolinecarbonitrile hydrate; Bosulif hydrate; KIN 001-160 hydrate; SK 606 hydrate; SKI 606 hydrate. Grade: 98%. CAS No. 918639-08-4. Molecular formula: C26H29Cl2N5O3.H2O. Mole weight: 548.46.
C086
C086 inhibits Hsp90 and BCR-ABL, resulting in decreased proliferation of tumor cells, including imatinib-resistant cells. Synonyms: C086; C 086; C-086. Grade: >98%. CAS No. 1160107-44-7. Molecular formula: C29H28O8. Mole weight: 504.53.
CGP 76030
CGP76030 is a ual-specific Src and Abl kinase inhibitor, inhibit growth and survival of cells expressing imatinib mesylate-resistant Bcr-Abl kinases. Uses: Ual-specific src and abl kinase inhibitor. Synonyms: CGP-76030; CGP76030; CGP76030; CGP-076030. 7-(4-(2-((2-methoxyethyl)amino)ethoxy)phenyl)-5-(3-methoxyphenyl)-7H-Pyrrolo(2,3-d)pyrimidin-4-amine. Grade: ≥98%. CAS No. 497152-38-2. Molecular formula: C24H27N5O3. Mole weight: 433.5.
Dasatinib
Dasatinib, also known as BMS-354825, is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. Dasatinib binds to and inhibits the growth-promoting activities of these kinases. Apparently because of its less stringent binding affinity for the BCR-ABL kinase, dasatinib has been shown to overcome the resistance to imatinib of chronic myeloid leukemia (CML) cells harboring BCR-ABL kinase domain point mutations. SRC-family protein-tyrosine kinases interact with variety of cell-surface receptors and participate in intracellular signal transduction pathways; tumorigenic forms can occur through altered regulation or expression of the endogenous protein and by way of virally-encoded kinase genes. Synonyms: BMS-354825; BMS354825; BMS354825. Grade: >98%. CAS No. 302962-49-8. Molecular formula: C22H26ClN7O2S. Mole weight: 488.01.
Dasatinib Free Base
Dasatinib, also known as BMS-354825, is a cancer drug produced by Bristol-Myers Squibb and sold under the trade name Sprycel. Dasatinib is an oral dual BCR/ABL and Src family tyrosine kinases inhibitor approved for use in patients with chronic myelogenous leukemia (CML) after imatinib treatment and Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL). It is also being assessed for use in metastatic melanoma. Group: Biochemicals. Alternative Names: N-[2-Chloro-6-methylphenyl]-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamide; BMS-354825. Grades: Highly Purified. CAS No. 302962-49-8. Pack Sizes: 100mg, 500mg. Molecular Formula: C22H26ClN7O2S, Molecular Weight: 488.01. US Biological Life Sciences.
Worldwide
DCC-2618
DCC-2618 inhibits normal and mutant KIT kinase at the nanomol level. The targets are wt c-KIT, c-KIT mutants, PDGFR alpha, PDGFR beta, KDR and cFMS. DCC-2618 inhibits mutant KIT in GIST patient cell line (GIST T1 pKIT western Ex11 deletion) at a IC 50 of 2 nM. Deciphera's technology has identified DCC-2618 as a molecule which can be developed as second line therapy for imatinib and sunitinib resistant GIST patients with the potential to progress to frontline GIST therapy. DCC-2618 has been designed to effectively inhibit the imatinib and sunitinib-sensitive KIT juxtamembrane domain mutants (JMD) as well as secondary resistant KIT kinase-domain mutants. DCC-2618 additionally targets PDGFR alpha oncogenic mutants. Synonyms: DCC2618; DCC 2618; c-Kit-IN-1; PDGFR inhibitor 1; N-[2,5-Difluoro-4-[[2-(1-methyl-1H-pyrazol-4-yl)-4-pyridinyl]oxy]phenyl]-N'-phenyl-1,1-cyclopropanedicarboxamide. Grade: >98%. CAS No. 1225278-16-9. Molecular formula: C26H21F2N5O3. Mole weight: 489.47.
Ethyl 2,4-Dimethylpyrrole-3-carboxylate
Ethyl 2,4-Dimethylpyrrole-3-carboxylate is an impurity of Sunitinib, which is an oral, small-molecule, multi-targeted receptor tyrosine kinase (RTK) inhibitor for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST). Synonyms: 1H-Pyrrole-3-carboxylic acid, 2,4-dimethyl-, ethyl ester; 2,4-Dimethyl-1H-pyrrole-3-carboxylic acid ethyl ester; 2,4-Dimethylpyrrole-3-carboxylic Acid Ethyl Ester; 2,4-Dimethyl-3-(ethoxycarbonyl)pyrrole; 2,4-Dimethyl-3-carbethoxypyrrole; 3-(Ethoxycarbonyl)-2,4-dimethylpyrrole; NSC 13425; Pyrrole-3-carboxylic acid, 2,4-dimethyl-, ethyl ester. Grade: ≥95%. CAS No. 2199-51-1. Molecular formula: C9H13NO2. Mole weight: 167.21.
Ethyl 5-Formyl-2,4-dimethylpyrrole-3-carboxylate
Ethyl 5-Formyl-2,4-dimethylpyrrole-3-carboxylate is an impurity of Sunitinib, which is an oral, small-molecule, multi-targeted receptor tyrosine kinase (RTK) inhibitor for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST). Synonyms: 5-Formyl-2,4-dimethyl-1H-pyrrole-3-carboxylic acid ethyl ester; Ethyl 5-formyl-2,4-dimethyl-1H-pyrrole-3-carboxylate; 2,4-Dimethyl-3-ethoxycarbonyl-5-formylpyrrole; 4-Ethoxycarbonyl-3,5-dimethylpyrrole-2-carboxaldehyde; 5-Formyl-2,4-dimethylpyrrole-3-carboxylic Acid Ethyl Ester; Ethyl 2,4-Dimethyl-5-formylpyrrole-3-carboxylate; Ethyl 2-Formyl-3,5-dimethylpyrrole-4-carboxylate; NSC 13426; 1H-Pyrrole-3-carboxylic acid, 5-formyl-2,4-dimethyl-, ethyl ester; Pyrrole-3-carboxylic acid, 5-formyl-2,4-dimethyl-, ethyl ester. Grade: ≥95%. CAS No. 2199-59-9. Molecular formula: C10H13NO3. Mole weight: 195.22.
Flumatinib Mesylate
Flumatinib mesylate, a derivative of imatinib, is a multi-kinase inhibitor for c-Abl, PDGFRβ and c-Kit. It is currently in Phase I and II clinical trials in China for the treatment of chronic myelogenous leukemia (CML). It effectively overcomes drug resistance of certain KIT mutants. It can reduce the expression of C-MYC, HIF-1 α and VEGF in U266 cell line in a time- and dose-dependent manners. Synonyms: HH-GV-678 mesylate. Grade: >98%. CAS No. 895519-91-2. Molecular formula: C30H33F3N8O4S. Mole weight: 658.69.
Icaritin is unable to promote proliferation, migration and tube-like structure formation by human umbilical vein endothelial cells (HUVECs) in vitro. Icaritin potently inhibited proliferation of K562 cells (IC50 was 8 μM) and primary CML cells (IC50 was 13.4 μM for CML-CP and 18 μM for CML-BC), induced CML cells apoptosis and promoted the erythroid differentiation of K562 cells with time-dependent manner. Furthermore, Icaritin was able to suppress the growth of primary CD34+ leukemia cells (CML) and Imatinib-resistant cells, and to induce apoptosis. Icaritin strongly inhibited the growth of breast cancer MDA-MB-453 and MCF7 cells. At concentrations of 2-3 μM, icaritin induced cell cycle arrest at the G(2)/M phase accompanied by a down-regulation of the expression levels of the G(2)/M regulatory proteins such as cyclinB, cdc2 and cdc25C. Icaritin at concentrations of 4-5 μM, however, induced apoptotic cell death characterized by the accumulation of the annexin V- and propidium iodide-positive cells, cleavage of poly ADP-ribose polymerase (PARP) and down-regulation of the Bcl-2 expression. In mouse leukemia model, Icaritin could prolong lifespan of NOD-SCID nude mice inoculated with K562 cells as effective as Imatinib without suppression of bone marrow. Icaritin could up-regulate phospho-JNK or phospho-C-Jun and down-regulate phospho-ERK, phospho-P-38, Jak-2, phospho-Stat3 and phospho-Akt expression with dose- or ti
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