Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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P167337-5mg | 5mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $70.90 | |
P167337-10mg | 10mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $105.90 | |
P167337-25mg | 25mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $177.90 | |
P167337-50mg | 50mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $284.90 | |
P167337-100mg | 100mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $497.90 | |
P167337-250mg | 250mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $1,120.90 | |
P167337-1g | 1g | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $4,033.90 |
Synonyms | (10R)-7-Amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-4,8-methenopyrazolo(4,3-h)(2,5,11)benzoxadiazacyclotetradecine-3-carbonitrile | NSC800990 | NSC-800990 | PFE-PKIS 10 | D70164 | BDBM50018830 | AKOS027250753 | Lorlatinib [USAN:INN] |
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Specifications & Purity | Moligand™, ≥98%(HPLC) |
Storage Temp | Store at -20°C,Argon charged |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | EML4-ALK inhibitor |
ALogP | 1.5 |
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IUPAC Name | (16R)-19-amino-13-fluoro-4,8,16-trimethyl-9-oxo-17-oxa-4,5,8,20-tetrazatetracyclo[16.3.1.02,6.010,15]docosa-1(22),2,5,10(15),11,13,18,20-octaene-3-carbonitrile |
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INCHI | InChI=1S/C21H19FN6O2/c1-11-15-7-13(22)4-5-14(15)21(29)27(2)10-16-19(17(8-23)28(3)26-16)12-6-18(30-11)20(24)25-9-12/h4-7,9,11H,10H2,1-3H3,(H2,24,25)/t11-/m1/s1 |
InChi Key | IIXWYSCJSQVBQM-LLVKDONJSA-N |
Canonical SMILES | CC1C2=C(C=CC(=C2)F)C(=O)N(CC3=NN(C(=C3C4=CC(=C(N=C4)N)O1)C#N)C)C |
Isomeric SMILES | C[C@@H]1C2=C(C=CC(=C2)F)C(=O)N(CC3=NN(C(=C3C4=CC(=C(N=C4)N)O1)C#N)C)C |
PubChem CID | 71731823 |
Molecular Weight | 406.41 |
PubChem CID | 71731823 |
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ChEMBL Ligand | CHEMBL3286830 |
CAS Registry No. | 1454846-35-5 |
RCSB PDB Ligand | 53P, 5P8, QB4 |
DrugCentral Ligand | 5302 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
---|---|---|---|
F23251452 | Certificate of Analysis | May 20, 2023 | P167337 |
F23251460 | Certificate of Analysis | May 20, 2023 | P167337 |
F23251490 | Certificate of Analysis | May 20, 2023 | P167337 |
F23251513 | Certificate of Analysis | May 20, 2023 | P167337 |
F23251520 | Certificate of Analysis | May 20, 2023 | P167337 |
F23251528 | Certificate of Analysis | May 20, 2023 | P167337 |
F23251540 | Certificate of Analysis | May 20, 2023 | P167337 |
Solubility | insoluble in H2O; ≥20.3 mg/mL in DMSO; ≥5.85 mg/mL in EtOH |
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Sensitivity | Moisture sensitive |
Pictogram(s) | GHS08, GHS09 |
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Signal | Warning |
Hazard Statements | H341:Suspected of causing genetic defects H373:Causes damage to organs through prolonged or repeated exposure H400:Very toxic to aquatic life H410:Very toxic to aquatic life with long lasting effects H361:Suspected of damaging fertility or the unborn child |
Precautionary Statements | P273:Avoid release to the environment. P280:Wear protective gloves/protective clothing/eye protection/face protection. P405:Store locked up. P501:Dispose of contents/container to ... P260:Do not breathe dust/fume/gas/mist/vapors/spray. P281:Use personal protective equipment as required. P391:Collect spillage. P203:Obtain, read and follow all safety instructions before use. P318:if exposed or concerned, get medical advice. P319:Get medical help if you feel unwell. |
1. Ye Zhongjiang, Wang Chenxiang, Li Rongqi, Chen Chuang, Yang Jianhui, Chen Yizhang, Fu Jing, Zhou Tao, Jin Mi, Huang Aifang, Zhang Xiuhua, Zhou Ziye. (2023) Potential interactions between triazole antifungal agents and lorlatinib based on ultra-performance liquid chromatography-tandem mass spectrometry in rat plasma. JOURNAL OF PHARMACY AND PHARMACOLOGY, 76 (2): (115-121). [PMID:38150242] |
1. Facchinetti F, Tiseo M, Di Maio M, Graziano P, Bria E, Rossi G, Novello S. (2016) Tackling ALK in non-small cell lung cancer: the role of novel inhibitors.. Transl Lung Cancer Res, 5 (3): (301-21). [PMID:27413712] |
2. Johnson TW, Richardson PF, Bailey S, Brooun A, Burke BJ, Collins MR, Cui JJ, Deal JG, Deng YL, Dinh D et al.. (2014) Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain exposure and broad-spectrum potency against ALK-resistant mutations.. J Med Chem, 57 (11): (4720-44). [PMID:24819116] |
3. Shaw AT, Friboulet L, Leshchiner I, Gainor JF, Bergqvist S, Brooun A, Burke BJ, Deng YL, Liu W, Dardaei L et al.. (2016) Resensitization to Crizotinib by the Lorlatinib ALK Resistance Mutation L1198F.. N Engl J Med, 374 (1): (54-61). [PMID:26698910] |
4. Shipman L. (2016) Resistance: Crizotinib makes a comeback.. Nat Rev Cancer, 16 (2): (69). [PMID:26797648] |
5. Zou HY, Li Q, Engstrom LD, West M, Appleman V, Wong KA, McTigue M, Deng YL, Liu W, Brooun A et al.. (2015) PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations.. Proc Natl Acad Sci USA, 112 (11): (3493-8). [PMID:25733882] |
6. Saha D, Kharbanda A, Yan W, Lakkaniga NR, Frett B, Li HY. (2020) The Exploration of Chirality for Improved Druggability within the Human Kinome.. J Med Chem, 63 (2): (441-469). [PMID:31550151] |
7. Ye Zhongjiang, Wang Chenxiang, Li Rongqi, Chen Chuang, Yang Jianhui, Chen Yizhang, Fu Jing, Zhou Tao, Jin Mi, Huang Aifang, Zhang Xiuhua, Zhou Ziye. (2023) Potential interactions between triazole antifungal agents and lorlatinib based on ultra-performance liquid chromatography-tandem mass spectrometry in rat plasma. JOURNAL OF PHARMACY AND PHARMACOLOGY, 76 (2): (115-121). [PMID:38150242] |