| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 100mg |
|
| ln Vitro |
Zidesamtinib (72 h), with average IC50s of 0.4 nM, inhibits the growth of seven cell lines expressing wild-type ROS1 fusions[1].
Zidesamtinib (72 h), with average IC50s of 1.6 nM, inhibits the growth of six cell lines harboring ROS1 fusions with the G2032R mutation[1]. Zidesamtinib (72 h) potently inhibits the non-G2032R ROS1 mutants, with IC50s ≤ 1.5 nM[1]. Zidesamtinib (10-1000 nM; 4 weeks) inhibits the formation of colonies in NIH3T3 cells that express both ROS1 fusions with G2032R and wild-type ROS1 fusions[1]. |
|---|---|
| ln Vivo |
Zidesamtinib (0.04-15 mg/kg; p.o. twice daily for 28 d) incites tumor regression in wild-type ROS1 xenograft models at all doses ≥0.2 mg/kg[1].
|
| Animal Protocol |
Female athymic Nude-Foxn1nu mice were implanted subcutaneously with tumor fragments from model CTG-0848[1]
0.04, 0.2, 1, 5, 15 mg/kg Oral gavage twice daily for 21 days |
| References |
| Molecular Formula |
C22H22FN7O
|
|---|---|
| Molecular Weight |
419.45
|
| Exact Mass |
419.460
|
| Elemental Analysis |
C, 63.00; H, 5.29; F, 4.53; N, 23.37; O, 3.81
|
| CAS # |
2739829-00-4
|
| Related CAS # |
2739829-00-4
|
| SMILES |
CCN1C2=C(CC3=NN(N=C3C4=C(C=C(C=C4)F)[C@H](OC5=C(N=CC2=C5)N)C)C)C=N1
|
| InChi Key |
DTWUUAFTYSMNQX-GFCCVEGCSA-N
|
| InChi Code |
InChI=1S/C22H22FN7O/c1-4-30-21-13(11-26-30)7-18-20(28-29(3)27-18)16-6-5-15(23)9-17(16)12(2)31-19-8-14(21)10-25-22(19)24/h5-6,8-12H,4,7H2,1-3H3,(H2,24,25)/t12-/m1/s1
|
| Chemical Name |
(19R)-3-ethyl-16-fluoro-10,19-dimethyl-20-oxa-3,4,9,10,11,23-hexazapentacyclo[19.3.1.02,6.08,12.013,18]pentacosa-1(25),2(6),4,8,11,13(18),14,16,21,23-decaen-22-amine
|
| Synonyms |
NVL520; NVL 520; NVL-520; Zidesamtinib
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~119.20 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.98 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (2.98 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.25 mg/mL (2.98 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3841 mL | 11.9204 mL | 23.8407 mL | |
| 5 mM | 0.4768 mL | 2.3841 mL | 4.7681 mL | |
| 10 mM | 0.2384 mL | 1.1920 mL | 2.3841 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
