Lorlatinib
- CAS No.
- 1454846-35-5
- Chemical Name:
- Lorlatinib
- Synonyms
- PF0643922;Loratinib;PF-06463922;PF-6463922;140539;CS-1727;PF6463922;Lorbrena.;EOS-60936;Laratinib
- CBNumber:
- CB02716543
- Molecular Formula:
- C21H19FN6O2
- Molecular Weight:
- 406.41
- MOL File:
- 1454846-35-5.mol
- MSDS File:
- SDS
- Modify Date:
- 2024/8/2 18:12:07
| Melting point | 184-187°C |
|---|---|
| Boiling point | 675.0±55.0 °C(Predicted) |
| Density | 1.42±0.1 g/cm3(Predicted) |
| storage temp. | Hygroscopic, -20°C Freezer, Under inert atmosphere |
| solubility | Chloroform (Slightly), Ethyl Acetate (Slightly) |
| form | Solid |
| pka | 6.05±0.40(Predicted) |
| color | White to Off-White |
| Stability | Hygroscopic |
| 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 |
| InChIKey | IIXWYSCJSQVBQM-LLVKDONJSA-N |
| SMILES | [C@@H]1(C)C2=CC(F)=CC=C2C(=O)N(C)CC2=NN(C)C(C#N)=C2C2C=C(C(N)=NC=2)O1 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS08 |
|---|---|
| Signal word | Warning |
| Hazard statements | H341-H373 |
| Precautionary statements | P260-P314-P501-P201-P202-P281-P308+P313-P405-P501 |
Lorlatinib Chemical Properties,Uses,Production
Uses
Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase that promotes cell proliferation and blocks apoptosis. PF-06463922 is an ATP-competitive, selective inhibitor of ALK (Ki = < 0.07 nM) and c-Ros oncogene 1 (ROS1, Ki = 0.7 nM). It has strong activity against all known ALK and ROS1 mutants identified in patients, including the EML4-L1196M mutant of ALK (Ki = < 0.02 nM). PF-06463922 is orally available, displaying inhibition of ALK phosphorylation and antitumor efficacy in a xenograft model expressing EML4-L1196M ALK. It demonstrates efficient blood-brain barrier penetration, produces brain tumor regression in mice harboring EML4-ALK tumors, and increases overall survival.[Cayman Chemical]
brand name
Lorbrena?
General Description
Class: receptor tyrosine kinase; Treatment: NSCLC; Oral bioavailability = 81%; Elimination half-life = 24 h; Protein binding = 66%
Enzyme inhibitor
This potent, dual ALK/ROS1 inhibitor (FW = 406.41 g/mol; CAS 1454846- 35-5), also named (10R)-7-amino-12-fluoro-10,15,16,17-tetrahydro- 2,10,16-trimethyl-15-oxo-2H-4,8-methenopyrazolo[4,3- h][2,5,11]benzoxadiazacyclotetradecine-3-carbonitrile, targets the protooncogene tyrosine-protein kinase ROS1 (Ki < 0.02 nM) as well as wild-type anaplastic lymphoma kinase ALKWT (Ki < 0.07 nM) and its Leu-to-Met mutant ALKL1196M (Ki of = 0.7 nM). PF-06463922 significantly inhibits cell proliferation and induces cell apoptosis in the HCC78 human NSCLC cells harboring SLC34A2-ROS1 fusions and the BaF3-CD74-ROS1 cells expressing human CD74-ROS1
target
Primary targets: ALK/ROS1
Lorlatinib Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| CLEARSYNTH LABS LTD. | +91-22-45045900 | Hyderabad, India | 6351 | 58 | Inquiry |
| A.J Chemicals | 91-9810153283 | New Delhi, India | 6124 | 58 | Inquiry |
| Pharmaffiliates Analytics and Synthetics P. Ltd | +91-172-5066494 | Haryana, India | 6773 | 58 | Inquiry |
| SynZeal Research Pvt Ltd | +1 226-802-2078 | Gujarat, India | 6522 | 58 | Inquiry |
| Pharma Affiliates | 172-5066494 | Haryana, India | 6761 | 58 | Inquiry |
| Shijiazhuang Dingmin Pharmaceutical Sciences Co., Ltd. | +86-0311-67591193 +8613931880626 | China | 251 | 58 | Inquiry |
| Zhengzhou Anhuida Chemical Co., Ltd | +8615903659408 | China | 297 | 58 | Inquiry |
| Henan Fengda Chemical Co., Ltd | +86-371-86557731 +86-13613820652 | China | 20294 | 58 | Inquiry |
| BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD. | +86-18600796368 +86-18600796368 | China | 212 | 58 | Inquiry |
| Capot Chemical Co.,Ltd. | 571-85586718 +8613336195806 | China | 29798 | 60 | Inquiry |
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