TPX-0005
Binding Mode- Product Name
- TPX-0005
- CAS No.
- 1802220-02-5
- Chemical Name
- TPX-0005
- Synonyms
- Repotrectinib;TPX-005;Ropotrectinib;CS-2479;TPX-0005;Loprotinib;PX0005(Ropotrectinib);TPX0005(Ropotrectinib);Repotrectinib,TPX-0005;TPX-0005,Repotrectinib
- CBNumber
- CB83312797
- Molecular Formula
- C18H18FN5O2
- Formula Weight
- 355.37
- MOL File
- 1802220-02-5.mol
TPX-0005 Property
- Density
- 1.46±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:35.0(Max Conc. mg/mL);98.5(Max Conc. mM)
Ethanol:10.0(Max Conc. mg/mL);28.1(Max Conc. mM) - form
- A crystalline solid
- pka
- 10.79±0.60(Predicted)
- color
- White to off-white
- InChI
- InChI=1S/C18H18FN5O2/c1-10-8-20-18(25)14-9-21-24-6-5-16(23-17(14)24)22-11(2)13-7-12(19)3-4-15(13)26-10/h3-7,9-11H,8H2,1-2H3,(H,20,25)(H,22,23)/t10-,11+/m0/s1
- InChIKey
- FIKPXCOQUIZNHB-WDEREUQCSA-N
- SMILES
- O1C2=CC=C(F)C=C2[C@@H](C)NC2C=CN3C(N=2)=C(C=N3)C(=O)NC[C@@H]1C
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 23397
- Product name
- TPX-0005
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 23397
- Product name
- TPX-0005
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $139
- Updated
- 2024/03/01
- Product number
- 23397
- Product name
- TPX-0005
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $243
- Updated
- 2024/03/01
- Product number
- 23397
- Product name
- TPX-0005
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $533
- Updated
- 2024/03/01
- Product number
- CS-7628
- Product name
- Repotrectinib
- Purity
- 99.81%
- Packaging
- 50mg
- Price
- $590
- Updated
- 2021/12/16
TPX-0005 Chemical Properties,Usage,Production
Binding Mode
The cocrystal structures of repotrectinib with TRK proteins are yet to be reported. However, a docking model with TRKA suggests that the pyrazole nitrogen forms hydrogen bonds with Met592 in the hinge area. The fluorophenyl group, positioned in a hydrophobic pocket, aligns perpendicularly to the macrocycle, and the lactam oxygen atom engages in a water-mediated hydrogen bond with Met592 in the hinge region (Figs. 1,2).
Description
Ropotrectinib (TPX-0005; TP Therapeutics, San Diego, CA, USA) is a nextgeneration ROS1 inhibitor, a novel three-dimensional macrocyle with a much smaller size (MW <370) than current ROS1 inhibitors. It was specifically designed to overcome resistance mutations. Preclinical studies have shown activity against gatekeeper and solvent mutations, including G2032R, D2033N, L2026M, S1986F/Y, L1951R, and kinases involved in bypass signaling such as focal adhesion kinase, SRC proto-oncogene, and non-receptor tyrosine kinase [102, 103].
Description
Repotrectinib, also known as TPX-0005, is a multikinase (ROS1, ALK, and TRKA/B/C) inhibitor that is tested in an ongoing first-in-human phase 1/2 trail (NCT03093116).
General Description
Class: receptor tyrosine kinase; Treatment: NSCLC; Other name: TPX-0005
Biological Activity
Repotrectinib is a potent inhibitor targeting solvent-front mutations (SFMs) of ROS1, pan-TRK, and ALK. It effectively inhibits the kinase activity of wild-type ROS1, TRKA-C, and ALK, along with their SFMs, with IC50 values ranging from 0.071 to 4.46 nM. The compound shows high potency against ROS1 and TRKA-C, with approximately 15-fold selectivity over ALK.
Clinical Use
Repotrectinib has advantage with central nervous system (CNS) penetration, aimed to target both wide-type (WT) and solvent-front mutations (SFM) kinases and other resistance mutations including ROS1-G2032R and ROS1-D2033N, TRKA-G595R, TRKB-G639R, TRKC-G623R, and ALK-G1202R.
target
Primary targets: NTRK, ROS, ALT
TPX-0005 Preparation Products And Raw materials
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View Lastest Price from TPX-0005 manufacturers
- Product
- Repotrectinib/TPX-0005 1802220-02-5
- Price
- US $2.00/kg
- Min. Order
- 1kg
- Purity
- 99%
- Supply Ability
- 50KG/M
- Release date
- 2023-08-14
- Product
- Repotrectinib 1802220-02-5
- Price
- US $0.00-0.00/kg
- Min. Order
- 1kg
- Purity
- 99%, Single impurity＜0.1
- Supply Ability
- 1 ton
- Release date
- 2023-12-20
- Product
- TPX-0005 1802220-02-5
- Price
- US $50.00/kg
- Min. Order
- 1kg
- Purity
- 0.99
- Supply Ability
- 10000
- Release date
- 2023-11-16