WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H577742
CAS#: Enbezotinib HCl
Description: Enbezotinib, also known as TPX-0046, is a novel and potent RET/SRC inhibitor for RET-driven cancers. In enzymatic assays, TPX-0046 demonstrated low nanomolar potency against WT and many mutated RETs, as well as SRC, and is VEGFR2-sparing. TPX-0046 potently inhibited RET phosphorylation and cell proliferation in in-house engineered Ba/F3 KIF5B-RET, TT, and LC2/ad cells with IC50s of approximately 1 nM. TPX-0046 is potent against the SFM G810R in Ba/F3 cell proliferation assay with a mean IC50 of 17 nM, whereas comparable proxy molecules for BLU-667 and LOXO-292 have IC50s >500 nM. TPX-0046 demonstrated marked anti-tumor efficacy in vivo in multiple RET-driven cancer cell-derived and patient-derived xenograft tumor models.
Hodoodo Cat#: H577742
Name: Enbezotinib HCl
CAS#: Enbezotinib HCl
Chemical Formula: C21H22ClFN6O3
Exact Mass: 0.00
Molecular Weight: 460.894
Elemental Analysis: C, 54.73; H, 4.81; Cl, 7.69; F, 4.12; N, 18.23; O, 10.41
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Related CAS #: 2359650-19-2 (SRR-isomer) 2359649-81-1 (RSS-isomer) Enbezotinib HCl,
Synonym: Enbezotinib HCl; TPX-0046; TPX 0046; TPX0046;
IUPAC/Chemical Name: (15aR,18aS,5S,E)-35-fluoro-5-methyl-13,13a,15,15a,16,17,18,18a-octahydro-4-oxa-7-aza-1(5,3)-cyclopenta[b]pyrazolo[1',5':1,2]pyrimido[4,5-e][1,4]oxazina-3(3,2)-pyridinacyclooctaphan-8-one hydrochloride
InChi Key: RPCVYVDIDPVRTO-XOYFWFMASA-N
InChi Code: InChI=1S/C21H21FN6O3.ClH/c1-11-6-23-20(29)14-8-25-28-10-17-19(26-18(14)28)27(15-3-2-4-16(15)31-17)9-12-5-13(22)7-24-21(12)30-11;/h5,7-8,10-11,15-16H,2-4,6,9H2,1H3,(H,23,29);1H/t11-,15+,16-;/m0./s1
SMILES Code: FC(C=C1CN2C3=NC4=C5C=NN4C=C3O[C@]6([H])[C@@]2([H])CCC6)=CN=C1O[C@@H](C)CNC5=O.[H]Cl
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
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The following data is based on the product molecular weight 460.89 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
