Larotrectinib Sulfate
Solubility- Product Name
- Larotrectinib Sulfate
- CAS No.
- 1223405-08-0
- Chemical Name
- Larotrectinib Sulfate
- Synonyms
- LOX-101;Loxo-101（S）;LOX-101(sulfate);ARRY 470) sulfate;LOXO-101 (sulfate);Larotrectinib sulfate;Larotrectinib(LOXO 101;ARRY-470, Larotrectinib;Larotrectinib sulfate salt;Larotrectinib sulfate（LOXO101）
- CBNumber
- CB93067010
- Molecular Formula
- C21H24F2N6O6S
- Formula Weight
- 526.52
- MOL File
- 1223405-08-0.mol
Larotrectinib Sulfate Property
- storage temp.
- Store at -20°C
- solubility
- ≥18.47 mg/mL in DMSO; ≥2.14 mg/mL in EtOH; ≥29.65 mg/mL in H2O
- form
- solid
- Stability:
- Hygroscopic
- InChI
- InChI=1/C21H22F2N6O2.H2O4S/c22-13-3-4-16(23)15(10-13)18-2-1-7-28(18)19-6-9-29-20(26-19)17(11-24-29)25-21(31)27-8-5-14(30)12-27;1-5(2,3)4/h3-4,6,9-11,14,18,30H,1-2,5,7-8,12H2,(H,25,31);(H2,1,2,3,4)/t14-,18+;/s3
- InChIKey
- PXHANKVTFWSDSG-RZOMTXEQNA-N
- SMILES
- S(O)(O)(=O)=O.FC1C=CC(F)=CC=1[C@H]1CCCN1C1C=CN2N=CC(NC(N3C[C@@H](O)CC3)=O)=C2N=1 |&1:13,29,r|
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
- L175933
- Product name
- LarotrectinibSulfate
- Packaging
- 100mg
- Price
- $55
- Updated
- 2021/12/16
- Product number
- CS-5314
- Product name
- Larotrectinibsulfate
- Purity
- 99.69%
- Packaging
- 5mg
- Price
- $60
- Updated
- 2021/12/16
- Product number
- B6176
- Product name
- LOXO-101
- Packaging
- 5mg
- Price
- $68
- Updated
- 2021/12/16
- Product number
- BL161518
- Product name
- Larotrectinib sulphate
- Packaging
- 10mg
- Price
- $90
- Updated
- 2021/12/16
- Product number
- CS-5314
- Product name
- Larotrectinibsulfate
- Purity
- 99.69%
- Packaging
- 10mg
- Price
- $100
- Updated
- 2021/12/16
Larotrectinib Sulfate Chemical Properties,Usage,Production
Solubility
LOXO-101 (sulfate) can be dissolved in DMSO(Slightly), Methanol (Slightly, Sonicated), Water (Slightly) .
Description
LOXO-101 (sulfate) (or Larotrectinib Sulfate) is an orally bioavailable, potent, ATP-competitive inhibitor of TRKA, TRKB, and TRKC. LOXO-101 has IC50 values in the low nanomolar range for inhibition of all three TRK family members in binding and cellular assays, with 100x selectivity over other kinases, and has shown acceptable pharmaceutical properties and safety in nonclinical models. The TRK family of neurotrophin receptors, TRKA, TRKB, and TRKC (encoded by NTRK1, NTRK2, and NTRK3 genes, respectively) and their neurotrophin ligands regulate growth, differentiation and survival of neurons.
Uses
Larotrectinib Sulfate is a potent and selective oral ATP-competitive inhibitor of tropomyosin receptor kinases (TRK).
Clinical Use
Larotrectinib sulfate is approved to treat solid tumors with NTRKgene fusion without drug resistance mutation in specific TRK proteins. It is used in adults and children whose cancer has metastasized (spread to other parts of the body) or cannot be removed by surgery and has gotten worse after other treatments or cannot be treated with other therapies. This use is approved under FDA’s Accelerated Approval Program. As a condition of approval, a confirmatory trial(s) must show that larotrectinib sulfate provides a clinical benefit in these patients. Larotrectinib sulfate is also being studied in treating other types of cancer.
in vitro
in previous study, loxo-101 was evaluated for off-target kinase enzyme inhibition against a panel of non-trk kinases at a concentration of 1,000 nm and atp concentrations around the km. results showed that loxo-101 had greater than 50% inhibition for only one non-trk kinase, which was tnk2 with ic50 of 576 nm. moreover, there were neither relevant herg inhibition nor prolonged qt observation [1].
in vivo
animal study found that loxo-101 was able to inhibit in vivo tumor growth. athymic nude mice injected with km12 cells were orally treated with loxo-101 daily for 2 weeks, and dose-dependent tumor inhibition was observed, indicating the ability of loxo-101 to inhibit in-vivo tumor growth [1].
IC 50
low nanomolar range for inhibition of all trk family members
References
[1] doebele rc et al. an oncogenic ntrk fusion in a patient with soft-tissue sarcoma with response to the tropomyosin-related kinase inhibitor loxo-101. cancer discov.2015 oct;5(10):1049-57.
Larotrectinib Sulfate Preparation Products And Raw materials
Raw materials
Preparation Products
Larotrectinib Sulfate Suppliers
- Tel
- 021-54156369 16621315851
- yhsuyiming@126.com
- Country
- China
- ProdList
- 306
- Advantage
- 58
- Tel
- 15342225168
- yutianchun2007@126.com
- Country
- China
- ProdList
- 10006
- Advantage
- 58
- Tel
- Fax
- 86-21-57758967
- sales@boylechem.com
- Country
- China
- ProdList
- 2923
- Advantage
- 55
- Tel
- 021-20908456
- Fax
- 021-58180499
- sales@BioChemBest.com
- Country
- China
- ProdList
- 6010
- Advantage
- 61
- Tel
- 0551-68779238 18056025720
- sales3@lcywhx.com
- Country
- China
- ProdList
- 168
- Advantage
- 57
- Tel
- 0411-62910999 13889544652
- sales@meilune.com
- Country
- China
- ProdList
- 4663
- Advantage
- 58
- Tel
- +21-18501659228 18501659228
- Fax
- sales@hope-chem.com
- info@hope-chem.com
- Country
- China
- ProdList
- 438
- Advantage
- 55
- Tel
- 021-58950125
- Fax
- (86) 21-58955996
- info@chemexpress.com
- Country
- China
- ProdList
- 7553
- Advantage
- 61
- Tel
- 020-39119399 18927568969
- Fax
- 020-39119999
- isunpharm@qq.com
- Country
- China
- ProdList
- 4428
- Advantage
- 55
- Tel
- 021-021-33632979 15002134094
- Fax
- 021-33632979
- marketing@targetmol.com
- Country
- China
- ProdList
- 7854
- Advantage
- 58
- Tel
- 86-21-37788339
- Fax
- 86-21-5768-0031
- Country
- China
- ProdList
- 76
- Advantage
- 55
- Tel
- 028-84502008 13568869383
- Fax
- 028-66476329
- sales@hygeiapharm.com
- Country
- China
- ProdList
- 296
- Advantage
- 55
- Tel
- 13120367189
- Fax
- 021-50315529
- mychess007@163.com
- Country
- China
- ProdList
- 1994
- Advantage
- 55
- Tel
- +86-571-87396432
- Fax
- 0571-87396431
- sales@jhechem.com
- Country
- China
- ProdList
- 10062
- Advantage
- 53
- Tel
- 021-60455363 18019463053
- Fax
- 50966098
- sales@coolpharm.com
- Country
- China
- ProdList
- 12357
- Advantage
- 58
- Tel
- 021-52996696，15000506266 15000506266
- Fax
- +86-21-52996696
- Country
- China
- ProdList
- 4182
- Advantage
- 55
- Tel
- 15066662237
- 3281004549@qq.com
- Country
- China
- ProdList
- 278
- Advantage
- 55
- Tel
- 021-61350663 13052117465
- Fax
- 021-61350662
- sales@zehanbiopharma.com
- Country
- China
- ProdList
- 990
- Advantage
- 55
- Tel
- 021-38751876 15000076078
- Fax
- 021-50275764
- Info@rochipharma.com
- Country
- China
- ProdList
- 561
- Advantage
- 55
- Tel
- 028-86040038 13980902949;
- Fax
- 028-85149890
- market@dingdangchem.com
- Country
- China
- ProdList
- 1755
- Advantage
- 55
- Tel
- 0531-88801869 15562622698
- Fax
- 0531-88801867
- sciencechem@163.com
- Country
- China
- ProdList
- 274
- Advantage
- 55
- Tel
- 021-65675885 18964387627
- Fax
- 021-65675885
- info@efebio.com
- Country
- China
- ProdList
- 9709
- Advantage
- 58
- Tel
- 021-31761238 13167072949
- Fax
- 021-31761238
- 3146446224@qq.com
- Country
- China
- ProdList
- 1611
- Advantage
- 55
- Tel
- 052386810091
- zcwy9518@yeah.net
- Country
- China
- ProdList
- 3871
- Advantage
- 58
- Tel
- 0317-5296180 15533709196
- Fax
- 0317-5106596
- sale@enkepharma.com
- Country
- China
- ProdList
- 1688
- Advantage
- 55
- Tel
- 17754423994 17754423994
- Fax
- QQ:2853530913
- 2853530910@QQ.com
- Country
- China
- ProdList
- 8011
- Advantage
- 62
- Tel
- 21-31433387 15618786686
- Fax
- QQ:1369748377
- sales@rechemscience.com
- Country
- China
- ProdList
- 2988
- Advantage
- 58
- Tel
- QQ:65489617 15618227136
- Fax
- 21-5161 9052
- info@SuperLan-chem.com
- Country
- China
- ProdList
- 9824
- Advantage
- 58
- Tel
- 021-2022843681 15618226720
- Fax
- +86-21-51601218
- chaolaichem@foxmail.com
- Country
- China
- ProdList
- 9242
- Advantage
- 58
- Tel
- 0371-0371-55629727 13323845623
- Fax
- 037155629727
- 2885676761@qq.com
- Country
- China
- ProdList
- 9859
- Advantage
- 58
- Tel
- 010-50973130 4009686088
- 3193328036@qq.com
- Country
- China
- ProdList
- 29796
- Advantage
- 68
- Tel
- 571-89925085
- Fax
- 0086-571-89925065
- sales@amadischem.com
- Country
- China
- ProdList
- 131980
- Advantage
- 58
- Tel
- 17836913271
- Fax
- 0374-8348899
- 3224305243@qq.com
- Country
- China
- ProdList
- 2790
- Advantage
- 58
- Tel
- 021-58180488
- Fax
- 021-58180499
- sales@MedChemLeader.com
- Country
- China
- ProdList
- 999
- Advantage
- 58
- Tel
- +86 18721201413
- Fax
- +86 (21) 5775-8967
- sales@biopharmaleader.com
- Country
- China
- ProdList
- 1720
- Advantage
- 58
- Tel
- 10106090
- jjlchem2@163.com
- Country
- China
- ProdList
- 9986
- Advantage
- 58
- Tel
- 0573-86-0573-85866609 13325730825
- Fax
- 0573-85866609
- 945717149@qq.com
- Country
- China
- ProdList
- 7960
- Advantage
- 58
- Tel
- 027-83778895 18602735115
- Fax
- 027-51119224
- 18602735115@163.com
- Country
- China
- ProdList
- 1999
- Advantage
- 64
- Tel
- 010-57862036 18811083386
- msales@mesochem.com
- Country
- China
- ProdList
- 191
- Advantage
- 58
- Tel
- 027-50476178
- Fax
- QQ644526144
- 644526144@qq.com
- Country
- China
- ProdList
- 418
- Advantage
- 58
- Tel
- Fax
- -
- jnyaoyan@163.com
- Country
- China
- ProdList
- 3069
- Advantage
- 58
- Tel
- 18550739526
- Fax
- QQ: 3394205705
- 3394205705@qq.com
- Country
- China
- ProdList
- 1752
- Advantage
- 58
- Tel
- 18068541569 18660163165
- Fax
- 0519-85551569
- sale@inyelchem.com
- Country
- China
- ProdList
- 194
- Advantage
- 58
- Tel
- 18895393626
- Fax
- -
- 3145613242@qq.com
- Country
- China
- ProdList
- 37
- Advantage
- 58
- Tel
- 028-85157043 15882256948
- 676046971@qq.com
- Country
- China
- ProdList
- 4394
- Advantage
- 58
- Tel
- 027-50478167
- Fax
- QQ 252994272
- 252994272@qq.com
- Country
- China
- ProdList
- 277
- Advantage
- 58
- Tel
- +8618229978283 18974947952
- sales@chemfish.com
- Country
- China
- ProdList
- 4907
- Advantage
- 58
- Tel
- 15911056312
- liming@bio-fount.com
- Country
- China
- ProdList
- 9730
- Advantage
- 58
- Tel
- 020-31155029 18902330969
- Fax
- 020-31155029
- sales@tomums.cn
- Country
- China
- ProdList
- 4698
- Advantage
- 58
- Tel
- 0571-85361029
- Fax
- 0571-85361029
- synstar518@163.com
- Country
- China
- ProdList
- 1991
- Advantage
- 58
View Lastest Price from Larotrectinib Sulfate manufacturers
- Product
- LOXO-101 (sulfate) 1223405-08-0
- Price
- US $0.00-0.00/kg
- Min. Order
- 1kg
- Purity
- 99%
- Supply Ability
- 100tons
- Release date
- 2023-08-16
- Product
- LOXO-101 1223405-08-0
- Price
- US $15.00-10.00/KG
- Min. Order
- 1KG
- Purity
- 99%+ HPLC
- Supply Ability
- Monthly supply of 1 ton
- Release date
- 2021-07-09
- Product
- LOXO-101 (sulfate) 1223405-08-0
- Price
- US $9.80/KG
- Min. Order
- 1g
- Purity
- ≥99%
- Supply Ability
- 100kg
- Release date
- 2020-01-08