2. Protein Tyrosine Kinase/RTK
  3. RET
  4. RET-IN-16

RET-IN-16 是一种有效且具有选择性的 RET 抑制剂，对 RET(WT)，RET(M918T)，RET(V804L)，RET(V804M)，RET-CCDC6 和 RET-KIF5B 的 IC50 分别为 3.98 nM，8.42 nM，15.05 nM，7.86 nM，5.43 nM 和 8.86 nM。RET-IN-16 具有抗癌作用。

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RET-IN-16 Chemical Structure

RET-IN-16 Chemical Structure

CAS No. : 2259657-48-0

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RET-IN-16 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

RET-IN-16 is a potent and selective RET inhibitor with IC50s of 3.98 nM, 8.42 nM, 15.05 nM, 7.86 nM, 5.43 nM and 8.86 nM for RET(WT), RET(M918T), RET(V804L), RET(V804M), RET-CCDC6 and RET-KIF5B, respectively. RET-IN-16 has anticancer effects[1].

IC50 & Target

IC50: 3.98 nM (RET(WT)), 8.42 nM (RET(M918T)), 15.05 nM (RET(V804L)), 7.86 nM (RET(V804M)), 5.43 nM (RET-CCDC6), 8.86 nM (RET-KIF5B)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A-375 GI50
2.947 μM
Compound: 9x
Antiproliferative activity against human A-375 cells measured after 48 hrs by MTS assay
Antiproliferative activity against human A-375 cells measured after 48 hrs by MTS assay
[PMID: 32882611]
A549 GI50
3.393 μM
Compound: 9x
Antiproliferative activity against human A549 cells measured after 48 hrs by MTS assay
Antiproliferative activity against human A549 cells measured after 48 hrs by MTS assay
[PMID: 32882611]
BaF3 GI50
8.03 μM
Compound: 9x
Cytotoxicity against mouse BaF3 cells assessed as reduction in cell proliferation measured after 48 hrs by MTS assay
Cytotoxicity against mouse BaF3 cells assessed as reduction in cell proliferation measured after 48 hrs by MTS assay
[PMID: 32882611]
MDA-MB-231 GI50
2.428 μM
Compound: 9x
Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by MTS assay
Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by MTS assay
[PMID: 32882611]
NCI-H3122 GI50
5.679 μM
Compound: 9x
Antiproliferative activity against human NCI-H3122 cells measured after 48 hrs by MTS assay
Antiproliferative activity against human NCI-H3122 cells measured after 48 hrs by MTS assay
[PMID: 32882611]
体外研究
(In Vitro)

RET-IN-16 (compound 9x) (0.005-10 μM; 48 hours) exhibits potent activity against CCDC6-RET-Ba/F3 and KIF5B-RET-Ba/F3 with GI50 of 9 nM and 17 nM, respectively[1].
RET-IN-16 (1 μM; 48 hours) selectively suppresses the proliferation of CCDC6-RET fusion cells[1].
RET-IN-16 (50 and 100 μM; 4 hours) remarkably blocks the autophosphorylation of RET in KIF5B-RET and KIF5B-RETV804M Ba/F3 cells, and the phosphorylation of the adapter protein SHC is also inhibited with a dose-dependent manner[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

RET-IN-16 相关抗体:

Cell Proliferation Assay

Cell Line: LC-2/ad, A549, H3122, MDA-MB-231 and A375, SKGT4, HepG2, KYSE450 and BGC823 cells[1]
Concentration: 1 μM
Incubation Time: 48 hours
Result: Potently suppressed the proliferation of LC-2/ad NSCLC cells harboring the CCDC6-RET fusion, but dramatically decreased potency against other RET-negative cancer cells.

Western Blot Analysis

Cell Line: KIF5B-RET and KIF5B-RETV804M Ba/F3 cells[1]
Concentration: 50 and 100 μM
Incubation Time: 4 hours
Result: Remarkably blocked the autophosphorylation of RET, and the phosphorylation of the adapter protein SHC was also inhibited in a dose-dependent manner.
体内研究
(In Vivo)

RET-IN-16 (1 mg/kg; IV; single) exhibits a good drug exposure (AUC0-t = 6959 ± 762 ng·h/mL) and a moderate half-life (T1/2 = 4.28 ± 0.43 h)[1].
RET-IN-16 (10 mg/kg; PO; single) exhibits a low maximum plasma concentration (Cmax = 194 ± 47 ng·h/mL) and drug exposure (AUC0-t = 2112 ± 117 ng·h/mL)[1].
RET-IN-16 (30 and 50 mg/kg; IV; daily; for 8 days) suppresses tumor growth in a dose-dependent manner, and significantly suppresses p-RET and p-SHC in both KIF5B-RET and KIF5B-RETV804M in tumor tissues, as well as significantly induces apoptosis in vivo[1].
Pharmacokinetic Parameters of RET-IN-16 in male Sprague-Dawley rats[1].

IV (1 mg/kg) PO (10 mg/kg)
T1/2 (h) 4.28 ± 0.43 7.59 ± 1.02
Tmax (h) 0.083 ± 0 0.75 ± 0.43
Cmax (ng/mL) 6097 ± 623 194 ± 47
AUC0-t (ng/mL·h) 6959 ± 762 2112 ± 117
AUC0-∞ (ng/mL·h) 7014 ± 753 2343 ± 157
F (%) 3.0

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats[1]
Dosage: 1 mg/kg for IV, 10 mg/kg for PO
Administration: IV and PO; single (Pharmacokinetic Analysis)
Result: Exhibited a good drug exposure (AUC0-t = 6959 ± 762 ng·h/mL) and a moderate half-life (T1/2 = 4.28 ± 0.43 h) at 1 mg/kg IV; observed a low maximum plasma concentration (Cmax = 194 ± 47 ng·h/mL) and drug exposure (AUC0-t = 2112 ± 117 ng·h/mL) at 10 mg/kg PO.
Animal Model: Half male and female BALB/c-nu mice (6-8 weeks; injected with KIF5B-RET Ba/F3 and KIF5B-RETV804M Ba/F3)[1]
Dosage: 30 and 50 mg/kg
Administration: IV; daily; for 8 days
Result: Suppressed tumor growth in a dose-dependent manner, and significantly suppressed p-RET and p-SHC in both KIF5B-RET and KIF5B-RETV804M in tumor tissues, as well as significantly induced apoptosis in vivo.
分子量

602.61

Formula

C31H29F3N8O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

RET-IN-16 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RET-IN-162259657-48-0RETAnticancerWTMutantOralV804MInhibitorinhibitorinhibit

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