Product Name :
Theliatinib
Description:
Theliatinib (HMPL-309) is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases. Anti-tumor activity.
CAS:
1353644-70-8
Molecular Weight:
442.51
Formula:
C25H26N6O2
Chemical Name:
(3aR,6aR)-N-4-[(3-ethynylphenyl)amino]-7-methoxyquinazolin-6-yl-1-methyl-octahydropyrrolo[2,3-c]pyrrole-5-carboxamide
Smiles :
CN1CC[C@@H]2CN(C[C@H]12)C(=O)NC1=CC2=C(NC3C=C(C=CC=3)C#C)N=CN=C2C=C1OC
InChiKey:
FSXCKIBROURMFT-VGSWGCGISA-N
InChi :
InChI=1S/C25H26N6O2/c1-4-16-6-5-7-18(10-16)28-24-19-11-21(23(33-3)12-20(19)26-15-27-24)29-25(32)31-13-17-8-9-30(2)22(17)14-31/h1,5-7,10-12,15,17,22H,8-9,13-14H2,2-3H3,(H,29,32)(H,26,27,28)/t17-,22+/m1/s1
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
Theliatinib (HMPL-309) is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases.Ezetimibe custom synthesis Anti-tumor activity.|Product information|CAS Number: 1353644-70-8|Molecular Weight: 442.51|Formula: C25H26N6O2|Chemical Name: (3aR,6aR)-N-4-[(3-ethynylphenyl)amino]-7-methoxyquinazolin-6-yl-1-methyl-octahydropyrrolo[2,3-c]pyrrole-5-carboxamide|Smiles: CN1CC[C@@H]2CN(C[C@H]12)C(=O)NC1=CC2=C(NC3C=C(C=CC=3)C#C)N=CN=C2C=C1OC|InChiKey: FSXCKIBROURMFT-VGSWGCGISA-N|InChi: InChI=1S/C25H26N6O2/c1-4-16-6-5-7-18(10-16)28-24-19-11-21(23(33-3)12-20(19)26-15-27-24)29-25(32)31-13-17-8-9-30(2)22(17)14-31/h1,5-7,10-12,15,17,22H,8-9,13-14H2,2-3H3,(H,29,32)(H,26,27,28)/t17-,22+/m1/s1|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 5 mg/mL (11.Plerixafor Epigenetics 30 mM; Need ultrasonic).PMID:33003957 |Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|Theliatinib significantly inhibits EGFR phosphorylation in A431 cells with an IC50 of 7 nM. Theliatinib also inhibits A431, H292 and FaDu cells survival with IC50 values of 80 nM, 58 nM and 354 nM, respectively.|In Vivo:|Theliatinib (2-15 mg/kg; oral administration;daily; for 21 days; NOD-SCID mice; PDECX 1T0950 model) treatment demonstrates tumor regression of 75% at the end of study, and with a dose response.|Products are for research use only. Not for human use.|
